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KIT Gene Record

  • Summary
  • Interactions
  • Claims
  • KIT 3815 Druggable GenomeClinically ActionableDrug Resistance

    Alternate Names:

    3815
    KIT PROTO-ONCOGENE RECEPTOR TYROSINE KINASE
    KIT
    C-Kit
    CD117
    PBT
    SCFR
    164920
    6342
    ENSG00000157404
    OTTHUMG00000128713
    Mast/stem cell growth factor receptor Kit
    Proto-oncogene c-Kit
    Tyrosine-protein kinase Kit
    p145 c-kit
    v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog
    Piebald trait protein
    CD_antigen=CD117
    BE0000453
    P10721
    KIT_HUMAN
    MAST/STEM CELL GROWTH FACTOR RECEPTOR PRECURSOR (EC 2.7.1.112) (SCFR) (PROTO-ONCOGENE TYROSINE-PROTEIN KINASE KIT) (C-KIT) (CD117 ANTIGEN). [SOURCE:UNIPROT/SWISSPROT;ACC:P10721]
    1805
    29
    NP_000213
    NM_000222
    KIT proto-oncogene, receptor tyrosine kinase
    PA30128
    T57700

    Gene Info:

    CancerCommons Reported Gene Name KIT
    CancerCommons Reported Gene Name VEGF, PDGF
    CancerCommons Reported Gene Name Receptor tyrosine kinases KIT, CSF1R, and FLT3
    Interpro Acc IPR001245
    Human Readable Name DRUGGABLE GENOME
    Interpro Type Domain
    Interpro Short Name Ser-Thr/Tyr_kinase_cat_dom
    Interpro Name Serine-threonine/tyrosine-protein kinase catalytic domain
    Uniprot Evidence 1: Evidence at protein level
    Uniprot Status Swiss-Prot
    Human Readable Name KINASE
    Initial Gene Query KIT
    Counted Citations from 1950-2000 7271
    Target Class Receptors
    Target Subclass EC:2.7.10.1
    Target Main Class Receptors
    Target Subclass PDGFR
    Target Subclass KInase
    Transmembrane Helix Count 1
    GuideToPharmacology Gene Category Name Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family
    GuideToPharmacology Gene Category ID 322
    Gene Biotype PROTEIN_CODING
    (29 More Sources)

    Gene Categories: Category Details

    KINASE
    TYROSINE KINASE
    DRUG RESISTANCE
    EXTERNAL SIDE OF PLASMA MEMBRANE
    DRUGGABLE GENOME
    CLINICALLY ACTIONABLE
    TRANSCRIPTION FACTOR

    Publications:

    Huynh et al., 2009, Sorafenib induces growth suppression in mouse models of gastrointestinal stromal tumor., Mol. Cancer Ther.
    Quintás-Cardama et al., 2008, Complete response of stage IV anal mucosal melanoma expressing KIT Val560Asp to the multikinase inhibitor sorafenib., Nat Clin Pract Oncol
    Allegra et al., 2014, A new KIT mutation (N505I) in acral melanoma confers constitutive signaling, favors tumorigenic properties, and is sensitive to imatinib., J. Invest. Dermatol.
    Lierman et al., 2007, The ability of sorafenib to inhibit oncogenic PDGFRbeta and FLT3 mutants and overcome resistance to other small molecule inhibitors., Haematologica
    Koch et al., 2006, Does the expression of c-kit (CD117) in neuroendocrine tumors represent a target for therapy?, Ann. N. Y. Acad. Sci.
    Heinrich et al., 2012, Sorafenib inhibits many kinase mutations associated with drug-resistant gastrointestinal stromal tumors., Mol. Cancer Ther.
    Schirosi et al., 2012, Activating c-KIT mutations in a subset of thymic carcinoma and response to different c-KIT inhibitors., Ann. Oncol.
    Guida et al., 2007, Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants., Clin. Cancer Res.
    Liu et al., 2006, Sorafenib blocks the RAF/MEK/ERK pathway, inhibits tumor angiogenesis, and induces tumor cell apoptosis in hepatocellular carcinoma model PLC/PRF/5., Cancer Res.
    Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics
    Woodman et al., 2009, Activity of dasatinib against L576P KIT mutant melanoma: molecular, cellular, and clinical correlates., Mol. Cancer Ther.
    Handolias et al., 2010, Clinical responses observed with imatinib or sorafenib in melanoma patients expressing mutations in KIT., Br. J. Cancer
    Guo et al., 2007, Sorafenib inhibits the imatinib-resistant KITT670I gatekeeper mutation in gastrointestinal stromal tumor., Clin. Cancer Res.
    Bisagni et al., 2009, Long lasting response to the multikinase inhibitor bay 43-9006 (Sorafenib) in a heavily pretreated metastatic thymic carcinoma., J Thorac Oncol
    Falchook et al., 2015, Dual antiangiogenic inhibition: a phase I dose escalation and expansion trial targeting VEGF-A and VEGFR in patients with advanced solid tumors., Invest New Drugs
    Cascone et al., 2007, Combined targeted therapies in non-small cell lung cancer: a winner strategy?, Curr Opin Oncol
    Dişel et al., 2011, Promising efficacy of sorafenib in a relapsed thymic carcinoma with C-KIT exon 11 deletion mutation., Lung Cancer
    Cannarile MA et al., 2017, Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy., J Immunother Cancer
    Kim et al., 2014, Increased KIT inhibition enhances therapeutic efficacy in gastrointestinal stromal tumor., Clin. Cancer Res.
    Valent et al., 2015, Chronic mast cell leukemia (MCL) with KIT S476I: a rare entity defined by leukemic expansion of mature mast cells and absence of organ damage., Ann. Hematol.
    Millward MJ et al., 2006, The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study., Br J Cancer
    Gotlib et al., 2016, Efficacy and Safety of Midostaurin in Advanced Systemic Mastocytosis., N. Engl. J. Med.
    Caenepeel et al., 2010, Motesanib inhibits Kit mutations associated with gastrointestinal stromal tumors., J. Exp. Clin. Cancer Res.
    Wasag et al., 2011, Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis., Exp. Hematol.
    Johnson et al., 2013, Hidden mastocytosis in acute myeloid leukemia with t(8;21)(q22;q22)., Am. J. Clin. Pathol.
    Marcucci G et al., 2020, Combination of dasatinib with chemotherapy in previously untreated core binding factor acute myeloid leukemia: CALGB 10801., Blood Adv
    Gajiwala et al., 2009, KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients., Proc. Natl. Acad. Sci. U.S.A.
    Gotlib et al., 2005, Activity of the tyrosine kinase inhibitor PKC412 in a patient with mast cell leukemia with the D816V KIT mutation., Blood
    Cairoli et al., 2006, Prognostic impact of c-KIT mutations in core binding factor leukemias: an Italian retrospective study., Blood
    Gleixner et al., 2007, Synergistic growth-inhibitory effects of two tyrosine kinase inhibitors, dasatinib and PKC412, on neoplastic mast cells expressing the D816V-mutated oncogenic variant of KIT., Haematologica
    Debiec-Rychter et al., 2005, Mechanisms of resistance to imatinib mesylate in gastrointestinal stromal tumors and activity of the PKC412 inhibitor against imatinib-resistant mutants., Gastroenterology
    Dizdar et al., 2008, Dasatinib may also inhibit c-Kit in triple negative breast cancer cell lines., Breast Cancer Res. Treat.
    Mpakou et al., 2013, Dasatinib inhibits proliferation and induces apoptosis in the KASUMI-1 cell line bearing the t(8;21)(q22;q22) and the N822K c-kit mutation., Leuk. Res.
    Carlino et al., 2014, Resistance to c-Kit inhibitors in melanoma: insights for future therapies., Oncoscience
    Ustun et al., 2009, Chemotherapy and dasatinib induce long-term hematologic and molecular remission in systemic mastocytosis with acute myeloid leukemia with KIT D816V., Leuk. Res.
    Emile et al., 2012, Frequencies of KIT and PDGFRA mutations in the MolecGIST prospective population-based study differ from those of advanced GISTs., Med. Oncol.
    Antonescu et al., 2007, L576P KIT mutation in anal melanomas correlates with KIT protein expression and is sensitive to specific kinase inhibition., Int. J. Cancer
    Smith et al., 2012, Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemia., Nature
    Pan et al., 2007, EXEL-0862, a novel tyrosine kinase inhibitor, induces apoptosis in vitro and ex vivo in human mast cells expressing the KIT D816V mutation., Blood
    Verstovsek et al., 2008, Phase II study of dasatinib in Philadelphia chromosome-negative acute and chronic myeloid diseases, including systemic mastocytosis., Clin. Cancer Res.
    Smith et al., 2013, The role of kinase inhibitors in the treatment of patients with acute myeloid leukemia., Am Soc Clin Oncol Educ Book
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Hong et al., 2012, [Secondary mutation of c-kit/PDGFRα genotypes after imatinib mesylate therapy and its relationship with efficacy of sunitinib]., Zhonghua Bing Li Xue Za Zhi
    Nakagomi et al., 2007, Juxtamembrane-type c-kit gene mutation found in aggressive systemic mastocytosis induces imatinib-resistant constitutive KIT activation., Lab. Invest.
    Carvajal et al., 2011, KIT as a therapeutic target in metastatic melanoma., JAMA
    Shah et al., 2006, Dasatinib (BMS-354825) inhibits KITD816V, an imatinib-resistant activating mutation that triggers neoplastic growth in most patients with systemic mastocytosis., Blood
    Schittenhelm et al., 2006, Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies., Cancer Res.
    Todd et al., 2013, Secondary c-Kit mutations confer acquired resistance to RTK inhibitors in c-Kit mutant melanoma cells., Pigment Cell Melanoma Res
    Tornillo et al., 2006, An update on molecular genetics of gastrointestinal stromal tumours., J. Clin. Pathol.
    Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer
    Ben-Ami et al., 2016, Long-term follow-up results of the multicenter phase II trial of regorafenib in patients with metastatic and/or unresectable GI stromal tumor after failure of standard tyrosine kinase inhibitor therapy., Ann. Oncol.
    Garner et al., 2014, Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients., Clin. Cancer Res.
    Foster et al., 2008, Association of paediatric mastocytosis with a polymorphism resulting in an amino acid substitution (M541L) in the transmembrane domain of c-KIT., Br. J. Dermatol.
    Rutkowski et al., 2007, Predictive factors for long-term effects of imatinib therapy in patients with inoperable/metastatic CD117(+) gastrointestinal stromal tumors (GISTs)., J. Cancer Res. Clin. Oncol.
    Growney et al., 2005, Activation mutations of human c-KIT resistant to imatinib mesylate are sensitive to the tyrosine kinase inhibitor PKC412., Blood
    Hirota et al., 1998, Gain-of-function mutations of c-kit in human gastrointestinal stromal tumors., Science
    McDonnell et al., 2011, V559A and N822I double KIT mutant melanoma with predictable response to imatinib?, Pigment Cell Melanoma Res
    Handolias et al., 2010, Mutations in KIT occur at low frequency in melanomas arising from anatomical sites associated with chronic and intermittent sun exposure., Pigment Cell Melanoma Res
    Spitaleri et al., 2015, Inactivity of imatinib in gastrointestinal stromal tumors (GISTs) harboring a KIT activation-loop domain mutation (exon 17 mutation pN822K)., Onco Targets Ther
    Zook et al., 2017, Combination of Imatinib Mesylate and AKT Inhibitor Provides Synergistic Effects in Preclinical Study of Gastrointestinal Stromal Tumor., Clin. Cancer Res.
    Li et al., 2015, FGFR-Mediated Reactivation of MAPK Signaling Attenuates Antitumor Effects of Imatinib in Gastrointestinal Stromal Tumors., Cancer Discov
    Patrikidou et al., 2016, Long-term outcome of molecular subgroups of GIST patients treated with standard-dose imatinib in the BFR14 trial of the French Sarcoma Group., Eur. J. Cancer
    Kitayama et al., 1995, Constitutively activating mutations of c-kit receptor tyrosine kinase confer factor-independent growth and tumorigenicity of factor-dependent hematopoietic cell lines., Blood
    Tamborini et al., 2004, A new mutation in the KIT ATP pocket causes acquired resistance to imatinib in a gastrointestinal stromal tumor patient., Gastroenterology
    Cameron et al., 2011, Ten Years of Treatment with 400 mg Imatinib per Day in a Case of Advanced Gastrointestinal Stromal Tumor., Case Rep Oncol
    Ströbel et al., 2004, Thymic carcinoma with overexpression of mutated KIT and the response to imatinib., N. Engl. J. Med.
    Jachetti et al., 2017, Imatinib Spares cKit-Expressing Prostate Neuroendocrine Tumors, whereas Kills Seminal Vesicle Epithelial-Stromal Tumors by Targeting PDGFR-β., Mol. Cancer Ther.
    Frost et al., 2002, Juxtamembrane mutant V560GKit is more sensitive to Imatinib (STI571) compared with wild-type c-kit whereas the kinase domain mutant D816VKit is resistant., Mol. Cancer Ther.
    Iurlo et al., 2014, Identification of kit(M541L) somatic mutation in chronic eosinophilic leukemia, not otherwise specified and its implication in low-dose imatinib response., Oncotarget
    Zeng S et al., 2017 Sep, Wnt/β-catenin Signaling Contributes to Tumor Malignancy and Is Targetable in Gastrointestinal Stromal Tumor., Mol Cancer Ther
    Girard et al., 2009, Comprehensive genomic analysis reveals clinically relevant molecular distinctions between thymic carcinomas and thymomas., Clin. Cancer Res.
    Hirota et al., 2001, Gain-of-function mutation at the extracellular domain of KIT in gastrointestinal stromal tumours., J. Pathol.
    Buti et al., 2011, Impressive response with imatinib in a heavily pretreated patient with metastatic c-KIT mutated thymic carcinoma., J. Clin. Oncol.
    Prenen et al., 2006, Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate., Clin. Cancer Res.
    Heinrich et al., 2017, Correlation of Long-term Results of Imatinib in Advanced Gastrointestinal Stromal Tumors With Next-Generation Sequencing Results: Analysis of Phase 3 SWOG Intergroup Trial S0033., JAMA Oncol
    Hartmann et al., 2005, Novel germline mutation of KIT associated with familial gastrointestinal stromal tumors and mastocytosis., Gastroenterology
    Guo et al., 2011, Phase II, open-label, single-arm trial of imatinib mesylate in patients with metastatic melanoma harboring c-Kit mutation or amplification., J. Clin. Oncol.
    Hagemann et al., 2014, Stabilization of disease after targeted therapy in a thymic carcinoma with KIT mutation detected by clinical next-generation sequencing., J Thorac Oncol
    Rossi et al., 2013, When a thymic carcinoma "becomes" a GIST., Lung Cancer
    Beadling et al., 2008, KIT gene mutations and copy number in melanoma subtypes., Clin. Cancer Res.
    Rapisuwon et al., 2014, Novel somatic KIT exon 8 mutation with dramatic response to imatinib in a patient with mucosal melanoma: a case report., Melanoma Res.
    Heinrich et al., 2008, Primary and secondary kinase genotypes correlate with the biological and clinical activity of sunitinib in imatinib-resistant gastrointestinal stromal tumor., J. Clin. Oncol.
    Conca et al., 2013, Are two better than one? A novel double-mutant KIT in GIST that responds to Imatinib., Mol Oncol
    Serrano et al., 2015, KRAS and KIT Gatekeeper Mutations Confer Polyclonal Primary Imatinib Resistance in GI Stromal Tumors: Relevance of Concomitant Phosphatidylinositol 3-Kinase/AKT Dysregulation., J. Clin. Oncol.
    Minor et al., 2012, Sunitinib therapy for melanoma patients with KIT mutations., Clin. Cancer Res.
    Curtin et al., 2006, Somatic activation of KIT in distinct subtypes of melanoma., J. Clin. Oncol.
    Debiec-Rychter et al., 2006, KIT mutations and dose selection for imatinib in patients with advanced gastrointestinal stromal tumours., Eur. J. Cancer
    Tefferi, 2009, Molecular drug targets in myeloproliferative neoplasms: mutant ABL1, JAK2, MPL, KIT, PDGFRA, PDGFRB and FGFR1., J. Cell. Mol. Med.
    Antonescu et al., 2005, Acquired resistance to imatinib in gastrointestinal stromal tumor occurs through secondary gene mutation., Clin. Cancer Res.
    Hodi et al., 2008, Major response to imatinib mesylate in KIT-mutated melanoma., J. Clin. Oncol.
    Terheyden et al., 2010, Response to imatinib mesylate depends on the presence of the V559A-mutated KIT oncogene., J. Invest. Dermatol.
    Heinrich et al., 2008, Correlation of kinase genotype and clinical outcome in the North American Intergroup Phase III Trial of imatinib mesylate for treatment of advanced gastrointestinal stromal tumor: CALGB 150105 Study by Cancer and Leukemia Group B and Southwest Oncology Group., J. Clin. Oncol.
    Hodi et al., 2013, Imatinib for melanomas harboring mutationally activated or amplified KIT arising on mucosal, acral, and chronically sun-damaged skin., J. Clin. Oncol.
    Carter et al., 2005, Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases., Proc. Natl. Acad. Sci. U.S.A.
    Heinrich et al., 2003, Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor., J. Clin. Oncol.
    Roberts et al., 2007, Resistance to c-KIT kinase inhibitors conferred by V654A mutation., Mol. Cancer Ther.
    Tuveson DA et al., 2001, STI571 inactivation of the gastrointestinal stromal tumor c-KIT oncoprotein: biological and clinical implications., Oncogene
    Dagher et al., 2002, Approval summary: imatinib mesylate in the treatment of metastatic and/or unresectable malignant gastrointestinal stromal tumors., Clin. Cancer Res.
    Pectasides et al., Complete response after imatinib mesylate administration in a patient with chemoresistant stage IV seminoma., Anticancer Res.
    Heinrich et al., 2006, Molecular correlates of imatinib resistance in gastrointestinal stromal tumors., J. Clin. Oncol.
    Lee et al., 2006, Response to imatinib in KIT- and PDGFRA-wild type gastrointestinal stromal associated with neurofibromatosis type 1., Dig. Dis. Sci.
    Goemans et al., 2005, Mutations in KIT and RAS are frequent events in pediatric core-binding factor acute myeloid leukemia., Leukemia
    Einhorn et al., 2006, Phase II study of imatinib mesylate in chemotherapy refractory germ cell tumors expressing KIT., Am. J. Clin. Oncol.
    Tamborini et al., 2006, Functional analyses and molecular modeling of two c-Kit mutations responsible for imatinib secondary resistance in GIST patients., Oncogene
    Dy et al., 2005, A phase II trial of imatinib (ST1571) in patients with c-kit expressing relapsed small-cell lung cancer: a CALGB and NCCTG study., Ann. Oncol.
    Gebreyohannes et al., 2016, Cabozantinib Is Active against Human Gastrointestinal Stromal Tumor Xenografts Carrying Different KIT Mutations., Mol. Cancer Ther.
    Posadas et al., 2007, A prospective analysis of imatinib-induced c-KIT modulation in ovarian cancer: a phase II clinical study with proteomic profiling., Cancer
    Tutone et al., 2011, Study of the role of "gatekeeper" mutations V654A and T670I of c-kit kinase in the interaction with inhibitors by means mixed molecular dynamics/docking approach., Bioinformation
    De Giorgi, 2007, KIT mutations and imatinib dose effects in patients with gastrointestinal stromal tumors., J. Clin. Oncol.
    Joensuu et al., 2017, Effect of KIT and PDGFRA Mutations on Survival in Patients With Gastrointestinal Stromal Tumors Treated With Adjuvant Imatinib: An Exploratory Analysis of a Randomized Clinical Trial., JAMA Oncol
    Kampa-Schittenhelm et al., 2013, Quizartinib (AC220) is a potent second generation class III tyrosine kinase inhibitor that displays a distinct inhibition profile against mutant-FLT3, -PDGFRA and -KIT isoforms., Mol. Cancer
    Joensuu, 2007, Second line therapies for the treatment of gastrointestinal stromal tumor., Curr Opin Oncol
    Quek R et al., 2009, Gastrointestinal stromal tumor: a clinical overview., Hematol Oncol Clin North Am
    Roskoski, 2007, Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor., Biochem. Biophys. Res. Commun.
    Barattè et al., 2004, Quantitation of SU1 1248, an oral multi-target tyrosine kinase inhibitor, and its metabolite in monkey tissues by liquid chromatograph with tandem mass spectrometry following semi-automated liquid-liquid extraction., J Chromatogr A
    Rutkowski et al., 2012, The outcome and predictive factors of sunitinib therapy in advanced gastrointestinal stromal tumors (GIST) after imatinib failure - one institution study., BMC Cancer
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Abrams et al., 2003, SU11248 inhibits KIT and platelet-derived growth factor receptor beta in preclinical models of human small cell lung cancer., Mol. Cancer Ther.
    Reichardt et al., 2016, Correlation of KIT and PDGFRA mutational status with clinical benefit in patients with gastrointestinal stromal tumor treated with sunitinib in a worldwide treatment-use trial., BMC Cancer
    Schueneman et al., 2003, SU11248 maintenance therapy prevents tumor regrowth after fractionated irradiation of murine tumor models., Cancer Res.
    Sonpavde et al., 2007, Pazopanib: a novel multitargeted tyrosine kinase inhibitor., Curr Oncol Rep
    Zhao et al., 2014, Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants., Cancer Sci.
    Cohen et al., 2015, Pharmacological Inhibition of KIT Activates MET Signaling in Gastrointestinal Stromal Tumors., Cancer Res.
    Wang et al., 2016, KIT Exon 11 Codons 557-558 Deletion Mutation Promotes Liver Metastasis Through the CXCL12/CXCR4 Axis in Gastrointestinal Stromal Tumors., Clin. Cancer Res.
    Shen et al., 2017, Inactivation of Receptor Tyrosine Kinases Reverts Aberrant DNA Methylation in Acute Myeloid Leukemia., Clin. Cancer Res.
    Delyon et al., 2017, STAT3 mediates Nilotinib response in KIT-altered Melanoma: a Phase II Multicenter Trial of the French Skin Cancer Network., J. Invest. Dermatol.
    Cullinane et al., 2010, Preclinical evaluation of nilotinib efficacy in an imatinib-resistant KIT-driven tumor model., Mol. Cancer Ther.
    Lee SJ et al., 2015, Phase II Trial of Nilotinib in Patients With Metastatic Malignant Melanoma Harboring KIT Gene Aberration: A Multicenter Trial of Korean Cancer Study Group (UN10-06)., Oncologist
    Sawaki et al., 2011, Phase 2 study of nilotinib as third-line therapy for patients with gastrointestinal stromal tumor., Cancer
    Cauchi et al., 2012, Evaluation of nilotinib in advanced GIST previously treated with imatinib and sunitinib., Cancer Chemother. Pharmacol.
    Guo et al., 2017, Efficacy and safety of nilotinib in patients with KIT-mutated metastatic or inoperable melanoma: final results from the global, single-arm, phase II TEAM trial., Ann. Oncol.
    Cho et al., 2012, Nilotinib in patients with metastatic melanoma harboring KIT gene aberration., Invest New Drugs
    Carvajal et al., 2015, Phase II Study of Nilotinib in Melanoma Harboring KIT Alterations Following Progression to Prior KIT Inhibition., Clin. Cancer Res.
    Jin et al., 2014, Ponatinib induces apoptosis in imatinib-resistant human mast cells by dephosphorylating mutant D816V KIT and silencing β-catenin signaling., Mol. Cancer Ther.
    1976, [Pathomechanisms and progress in the therapy of hypertension. 4. Hannover Nephrological Symposium]., Med Monatsschr
    Gozgit et al., 2011, Potent activity of ponatinib (AP24534) in models of FLT3-driven acute myeloid leukemia and other hematologic malignancies., Mol. Cancer Ther.
    Huang et al., 2010, Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant., J. Med. Chem.
    Lierman et al., 2012, Ponatinib is active against imatinib-resistant mutants of FIP1L1-PDGFRA and KIT, and against FGFR1-derived fusion kinases., Leukemia
    Aghajanian, 1976, LSD and 2-bromo-LSD: comparison on effects on serotonergic neurones and on neurones in two serotonergic projection areas, the ventral lateral geniculate and amygdala., Neuropharmacology
    Gleixner et al., 2013, Synergistic growth-inhibitory effects of ponatinib and midostaurin (PKC412) on neoplastic mast cells carrying KIT D816V., Haematologica
    Silen et al., 1975, Acid-base balance in amphibian gastric mucosa., Am. J. Physiol.
    Matsui et al., 2008, E7080, a novel inhibitor that targets multiple kinases, has potent antitumor activities against stem cell factor producing human small cell lung cancer H146, based on angiogenesis inhibition., Int. J. Cancer
    Wu CP et al., 2019, Avapritinib: A Selective Inhibitor of KIT and PDGFRα that Reverses ABCB1 and ABCG2-Mediated Multidrug Resistance in Cancer Cell Lines., Mol Pharm
    Zick et al., 2017, Treatment inferred from mutations identified using massive parallel sequencing leads to clinical benefit in some heavily pretreated cancer patients., Medicine (Baltimore)
    Mahadevan et al., 2007, A novel tyrosine kinase switch is a mechanism of imatinib resistance in gastrointestinal stromal tumors., Oncogene
    Liu P et al., 2020, The Use of Molecular Subtypes for Precision Therapy of Recurrent and Metastatic Gastrointestinal Stromal Tumor., Onco Targets Ther
    Nemunaitis J et al., 2020, Intrigue: Phase III study of ripretinib versus sunitinib in advanced gastrointestinal stromal tumor after imatinib., Future Oncol
    Rönnstrand L, 2004, Signal transduction via the stem cell factor receptor/c-Kit., Cell Mol Life Sci
    Rolf MG et al., 2015, In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib., Pharmacol Res Perspect
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
  • AVAPRITINIB   KIT

    Interaction Score: 2.24

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type gastrointestinal stromal tumor
    Response Type sensitive
    Approval Status Phase I

    PMIDs:
    31117741


    Sources:
    OncoKB JAX-CKB TTD DrugBank GuideToPharmacology

  • QUIZARTINIB   KIT

    Interaction Score: 1.58

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Pathway activation
    Clinical Status preclinical
    Variant Effect gain-of-function

    PMIDs:
    23497317 21689725 24045550 19164557 15972446 16384925 18024392 18986703 22504184 16912224 23714533 25157968 17259998 23582185 16731599


    Sources:
    DoCM JAX-CKB GuideToPharmacology ChemblInteractions

  • ANCESTIM   KIT

    Interaction Score: 1.49

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:

    PMIDs:
    15526160


    Sources:
    DrugBank

  • NILOTINIB   KIT

    Interaction Score: 1.26

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Melanoma
    Indication/Tumor Type melanoma
    Response Type sensitive

    PMIDs:
    28720666 28843487 20442311 25594040 26424760 21456006 17372901 25209843 22119758 28327988 22068222 25695690 19671763 17699867 23582185


    Sources:
    CancerCommons MyCancerGenomeClinicalTrial JAX-CKB CIViC DrugBank COSMIC CGI

  • IMATINIB   KIT

    Interaction Score: 1.1

    Interaction Types & Directionality:
    multitarget
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Approval Status Guideline
    Indication/Tumor Type prostate neuroendocrine neoplasm
    Approval Status Phase II

    PMIDs:
    18795925 17458563 15790786 9438854 21159146 21689725 20088873 26316776 24045550 27370604 18936790 24317392 25673643 26687836 7530509 15236194 19164557 22114577 15201427 15972446 16384925 18024392 27980106 12481435 15685537 25015329 28611108 19861435 11276010 25594040 21969494 16638875 28196207 18986703 21953054 16143141 21690468 24419427 23375402 18980976 22357254 17372901 22504184 25003536 18955458 23567324 24687822 22261812 16908931 16624552 19175693 16912224 25239608 15930355 18421059 19812602 18955451 23775962 23714533 19671763 25157968 20372153 16046538 17699867 22932406 14645423 17363509 11526490 17259998 12374669 21642685 18751412 16954519 16865565 16015387 16462496 16434489 16751810 16087693 23582185 27777285 17559139 22355224 17369583 28334365 16731599


    Sources:
    TEND OncoKB FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TTD DrugBank COSMIC TALC MyCancerGenome CGI

  • CHEMBL286939   KIT

    Interaction Score: 0.75

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17139284 17016423


    Sources:
    DrugBank

  • RIPRETINIB   KIT

    Interaction Score: 0.75

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type gastrointestinal stromal tumor
    Response Type predicted – sensitive
    Approval Status Phase I

    PMIDs:
    32273716 31755321


    Sources:
    JAX-CKB TTD DrugBank GuideToPharmacology

  • AMG-191   KIT

    Interaction Score: 0.75

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • SUNITINIB   KIT

    Interaction Score: 0.64

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Alteration KIT:449-514,550-592,627-664,664-714,788-828
    Alteration KIT:788-828
    Alteration KIT:Y553N

    PMIDs:
    19164557 17545799 19248971 19861435 25594040 21969494 17367763 16638875 21690468 23375402 22357254 18955458 22261812 25239608 14753710 22439647 11752352 18421059 21642685 12748309 23582185 26772734 12873999


    Sources:
    MyCancerGenomeClinicalTrial TEND OncoKB PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC TALC MyCancerGenome GuideToPharmacology CGI

  • AMUVATINIB   KIT

    Interaction Score: 0.64

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name MP-470
    Novel drug target Established target
    Mechanism of Interaction Stem cell growth factor receptor inhibitor

    PMIDs:
    17325667


    Sources:
    TdgClinicalTrial DrugBank TALC MyCancerGenome ChemblInteractions

  • MOTESANIB   KIT

    Interaction Score: 0.56

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Direct Interaction yes
    Notes

    PMIDs:
    20633291


    Sources:
    JAX-CKB TdgClinicalTrial TALC MyCancerGenome ChemblInteractions

  • PEXIDARTINIB   KIT

    Interaction Score: 0.52

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type gastrointestinal stromal tumor
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    28716061 24583793


    Sources:
    CancerCommons JAX-CKB TTD DrugBank MyCancerGenome GuideToPharmacology ChemblInteractions

  • OSI-930   KIT

    Interaction Score: 0.43

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction The IC50 varied dependent on whether KIT was activated or unactivated, with the lower value measured for the activated enzyme.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    TTD DrugBank GuideToPharmacology ChemblInteractions

  • PONATINIB   KIT

    Interaction Score: 0.37

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Drug family BCR-ABL inhibitor 3rd gen&Pan-TK inhibitor
    Alteration KIT:788-828,829-860,550-592
    Alteration KIT:A829P,V654A,T670I

    PMIDs:
    24552773 10517 21482694 20513156 22301675 25239608 10535 23539538 2015


    Sources:
    DTC JAX-CKB CIViC TTD DrugBank CGI

  • TELATINIB   KIT

    Interaction Score: 0.37

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Direct Interaction yes
    Notes

    PMIDs:
    None found


    Sources:
    TALC MyCancerGenome ChemblInteractions

  • AKN-028   KIT

    Interaction Score: 0.37

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? True
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • DASATINIB   KIT

    Interaction Score: 0.36

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Melanoma
    Clinical Status preclinical
    Clinical Status early trials

    PMIDs:
    21689725 24045550 32092139 19164557 15972446 16384925 18024392 15685537 17351742 23149070 25594040 18986703 21953054 17372901 22504184 16912224 18559612 23714533 19671763 25157968 17699867 22932406 17259998 21642685 16434489 16397263 23582185 16731599


    Sources:
    CancerCommons MyCancerGenomeClinicalTrial TEND DoCM JAX-CKB TdgClinicalTrial CIViC DrugBank TALC ChemblInteractions CGI

  • REGORAFENIB   KIT

    Interaction Score: 0.35

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Response Type decreased response
    Approval Status Preclinical - Cell culture
    Approval Status Phase II

    PMIDs:
    21170960 27371698 25239608


    Sources:
    MyCancerGenomeClinicalTrial OncoKB JAX-CKB CIViC TTD DrugBank TALC MyCancerGenome ChemblInteractions CGI

  • FAMITINIB   KIT

    Interaction Score: 0.32

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology ChemblInteractions

  • MASITINIB   KIT

    Interaction Score: 0.32

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? True

    PMIDs:
    None found


    Sources:
    CancerCommons MyCancerGenomeClinicalTrial TdgClinicalTrial MyCancerGenome GuideToPharmacology ChemblInteractions

  • MIDOSTAURIN   KIT

    Interaction Score: 0.29

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type mast-cell leukemia
    Response Type predicted – sensitive
    Approval Status Preclinical - Patient cell culture

    PMIDs:
    25209843 16969355 27355533


    Sources:
    FDA PharmGKB JAX-CKB CIViC DrugBank MyCancerGenome ChemblInteractions

  • TANDUTINIB   KIT

    Interaction Score: 0.27

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    DTC MyCancerGenome GuideToPharmacology ChemblInteractions

  • SORAFENIB   KIT

    Interaction Score: 0.26

    Interaction Types & Directionality:
    antagonist (inhibitory)
    inhibitor (inhibitory)

    Interaction Info:
    Drug family Pan-TK inhibitor
    Alteration KIT:550-592,627-664,788-828,829-860
    Alteration KIT:D820E

    PMIDs:
    19139124 18936790 24317392 17229632 17102120 22665524 22357254 17545544 17178882 28362716 19671763 20372153 17699867 19461405 25363205 17272980 20970876


    Sources:
    TEND OncoKB PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC TTD DrugBank TALC MyCancerGenome GuideToPharmacology CGI

  • EDICOTINIB   KIT

    Interaction Score: 0.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • HENATINIB   KIT

    Interaction Score: 0.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • FLUMATINIB   KIT

    Interaction Score: 0.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • XL-820   KIT

    Interaction Score: 0.25

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • CABOZANTINIB   KIT

    Interaction Score: 0.23

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Indication/Tumor Type gastrointestinal stromal tumor
    Response Type sensitive
    Approval Status Preclinical

    PMIDs:
    24205792 25836719 27777285


    Sources:
    JAX-CKB MyCancerGenome

  • VATALANIB   KIT

    Interaction Score: 0.23

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name vatalanib, PTK 787
    Novel drug target Established target
    Trial Name Vatalanib

    PMIDs:
    None found


    Sources:
    DTC TdgClinicalTrial TALC ChemblInteractions

  • AXITINIB   KIT

    Interaction Score: 0.21

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name axitinib, AG-013736
    Novel drug target Established target
    Reported Cancer Type Prostate

    PMIDs:
    None found


    Sources:
    CancerCommons TdgClinicalTrial TALC MyCancerGenome

  • CM-082   KIT

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • RIVOCERANIB   KIT

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Assay used apatinib mesylate (YN968D1)
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CHEMBL1908396   KIT

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • SU-014813   KIT

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • CHEMBL406375   KIT

    Interaction Score: 0.19

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? True
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • LENVATINIB   KIT

    Interaction Score: 0.16

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Trial Name E7080
    Novel drug target Established target

    PMIDs:
    17943726


    Sources:
    TdgClinicalTrial DrugBank

  • ANLOTINIB   KIT

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • IMATINIB MESYLATE   KIT

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • CHEMBL1908395   KIT

    Interaction Score: 0.15

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • PD-0325901   KIT

    Interaction Score: 0.14

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type gastrointestinal stromal tumor
    Response Type sensitive
    Approval Status Preclinical - Cell culture

    PMIDs:
    26936919


    Sources:
    JAX-CKB

  • PAZOPANIB   KIT

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    17288876


    Sources:
    MyCancerGenomeClinicalTrial DrugBank TALC MyCancerGenome GuideToPharmacology

  • SEMAXANIB   KIT

    Interaction Score: 0.1

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    GuideToPharmacology ChemblInteractions

  • CRENOLANIB   KIT

    Interaction Score: 0.09

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • ROMIPLOSTIM   KIT

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • MK-2206   KIT

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Imatinib + MK2206
    Indication/Tumor Type gastrointestinal stromal tumor
    Response Type sensitive

    PMIDs:
    27370604


    Sources:
    JAX-CKB

  • SUNITINIB MALATE   KIT

    Interaction Score: 0.08

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Stem cell growth factor receptor inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • BARASERTIB   KIT

    Interaction Score: 0.08

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • XL-999   KIT

    Interaction Score: 0.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • PEMBROLIZUMAB   KIT

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Pembrolizumab + Trametinib
    Indication/Tumor Type melanoma
    Response Type no benefit

    PMIDs:
    28514312


    Sources:
    JAX-CKB

  • PAZOPANIB HYDROCHLORIDE   KIT

    Interaction Score: 0.07

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Stem cell growth factor receptor inhibitor

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • INFIGRATINIB   KIT

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy BGJ398 + Imatinib
    Indication/Tumor Type gastrointestinal stromal tumor
    Response Type sensitive

    PMIDs:
    25673643


    Sources:
    JAX-CKB

  • LUCITANIB   KIT

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • ENMD-2076   KIT

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Novel drug target Established target

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial ChemblInteractions

  • ERDAFITINIB   KIT

    Interaction Score: 0.06

    Interaction Types & Directionality:
    substrate

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DrugBank

  • SITRAVATINIB   KIT

    Interaction Score: 0.06

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction In a biochemical enzyme activity assay.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • FORETINIB   KIT

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • SORAFENIB TOSYLATE   KIT

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • CEDIRANIB   KIT

    Interaction Score: 0.05

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    TALC GuideToPharmacology ChemblInteractions

  • AST-487   KIT

    Interaction Score: 0.04

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology

  • BEVACIZUMAB   KIT

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Bevacizumab + Sorafenib
    Indication/Tumor Type gastrointestinal stromal tumor
    Response Type sensitive

    PMIDs:
    25363205


    Sources:
    JAX-CKB

  • CYTARABINE   KIT

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Dasatinib + Cytarabine
    Indication/Tumor Type acute myeloid leukemia
    Response Type sensitive

    PMIDs:
    18986703


    Sources:
    JAX-CKB

  • TRAMETINIB   KIT

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Clinical Study
    Response Type no benefit

    PMIDs:
    28514312


    Sources:
    JAX-CKB

  • DOVITINIB   KIT

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Mechanism of Interaction Stem cell growth factor receptor inhibitor
    Direct Interaction yes
    Specific Action of the Ligand Inhibition

    PMIDs:
    None found


    Sources:
    ClearityFoundationClinicalTrial DTC GuideToPharmacology ChemblInteractions

  • LINIFANIB   KIT

    Interaction Score: 0.03

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    TdgClinicalTrial DrugBank GuideToPharmacology

  • CHEMBL578061   KIT

    Interaction Score: 0.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CHEMBL541400   KIT

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CENISERTIB   KIT

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes

    PMIDs:
    None found


    Sources:
    DTC TALC MyCancerGenome

  • GW843682X   KIT

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SNS-314   KIT

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • RG-1530   KIT

    Interaction Score: 0.02

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False
    Direct Interaction? False

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology

  • JNJ-7706621   KIT

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ILORASERTIB   KIT

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Measuring inhibition of kinase activity in a biochemical assay.
    Specific Action of the Ligand Inhibition
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    DTC GuideToPharmacology

  • ENTRECTINIB   KIT

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • SP-600125   KIT

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • CYC-116   KIT

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • FOSTAMATINIB   KIT

    Interaction Score: 0.01

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    26516587


    Sources:
    DrugBank

  • Ensembl: ENSG00000157404

    • Version: 101_38

    Alternate Names:
    KIT Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • RussLampel: ENSG00000157404

    • Version: 26-July-2011

    Alternate Names:
    MAST/STEM CELL GROWTH FACTOR RECEPTOR PRECURSOR (EC 2.7.1.112) (SCFR) (PROTO-ONCOGENE TYROSINE-PROTEIN KINASE KIT) (C-KIT) (CD117 ANTIGEN). [SOURCE:UNIPROT/SWISSPROT;ACC:P10721] Description
    KIT Display Id
    ENSG00000157404 Ensembl Gene Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • BaderLabGenes: KIT

    • Version: February-2014

    Alternate Names:
    3815 Entrez Gene ID

    Gene Info:
    Initial Gene Query KIT
    Counted Citations from 1950-2000 7271

    Gene Categories:
    KINASE

    Publications:

  • HopkinsGroom: P10721

    • Version: 11-September-2012

    Alternate Names:
    MAST/STEM CELL GROWTH FACTOR RECEPTOR KIT Uniprot Protein Name
    KIT_HUMAN Uniprot Id
    P10721 Uniprot Accession

    Gene Info:
    Interpro Acc IPR001245
    Human Readable Name DRUGGABLE GENOME
    Interpro Type Domain

    Gene Categories:
    KINASE, DRUGGABLE GENOME

    Publications:

  • TdgClinicalTrial: P10721

    • Version: January-2014

    Alternate Names:
    KIT Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass EC:2.7.10.1

    Publications:

  • TEND: P10721

    • Version: 01-August-2011

    Alternate Names:
    3815 Entrez Gene Id
    P10721 Uniprot Accession
    KIT_HUMAN Uniprot Id

    Gene Info:
    Target Main Class Receptors
    Target Subclass PDGFR
    Target Subclass KInase

    Publications:

  • CancerCommons: KIT

    • Version: 25-July-2013

    Alternate Names:
    3815 Entrez Gene ID

    Gene Info:
    CancerCommons Reported Gene Name KIT
    CancerCommons Reported Gene Name VEGF, PDGF
    CancerCommons Reported Gene Name Receptor tyrosine kinases KIT, CSF1R, and FLT3

    Publications:

  • GuideToPharmacology: 3815

    • Version: 29-September-2020

    Alternate Names:
    6342 HUGO Gene ID
    6342 HUGO Gene Symbol
    KIT proto-oncogene, receptor tyrosine kinase HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family
    GuideToPharmacology Gene Category ID 322

    Publications:

  • JAX-CKB: KIT

    • Version: 27-September-2017

    Alternate Names:
    3815 CKB Entrez Id
    KIT CKB Gene Synonym
    C-Kit CKB Gene Synonym

    Gene Info:

    Publications:
    Wilhelm et al., 2011, Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity., Int. J. Cancer
    Ben-Ami et al., 2016, Long-term follow-up results of the multicenter phase II trial of regorafenib in patients with metastatic and/or unresectable GI stromal tumor after failure of standard tyrosine kinase inhibitor therapy., Ann. Oncol.
    Garner et al., 2014, Ponatinib inhibits polyclonal drug-resistant KIT oncoproteins and shows therapeutic potential in heavily pretreated gastrointestinal stromal tumor (GIST) patients., Clin. Cancer Res.

  • PharmGKB: KIT

    • Version: 18-August-2020

    Alternate Names:
    PA30128 PharmGKB ID

    Gene Info:

    Publications:
    Tuveson DA et al., 2001, STI571 inactivation of the gastrointestinal stromal tumor c-KIT oncoprotein: biological and clinical implications., Oncogene
    Quek R et al., 2009, Gastrointestinal stromal tumor: a clinical overview., Hematol Oncol Clin North Am
    Gong L et al., 2017, PharmGKB summary: sorafenib pathways., Pharmacogenet Genomics

  • CIViC: KIT

    • Version: 14-September-2020

    Alternate Names:
    3815 Entrez Gene ID
    29 CIViC Gene ID

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE

    Publications:
    Woodman et al., 2009, Activity of dasatinib against L576P KIT mutant melanoma: molecular, cellular, and clinical correlates., Mol. Cancer Ther.
    Guo et al., 2007, Sorafenib inhibits the imatinib-resistant KITT670I gatekeeper mutation in gastrointestinal stromal tumor., Clin. Cancer Res.
    Bisagni et al., 2009, Long lasting response to the multikinase inhibitor bay 43-9006 (Sorafenib) in a heavily pretreated metastatic thymic carcinoma., J Thorac Oncol

  • DrugBank: BE0000453

    • Version: 5.1.7

    Alternate Names:
    KIT DrugBank Gene Name
    P10721 UniProt Accession
    3815 Entrez Gene Id

    Gene Info:

    Publications:
    Lierman et al., 2007, The ability of sorafenib to inhibit oncogenic PDGFRbeta and FLT3 mutants and overcome resistance to other small molecule inhibitors., Haematologica
    Koch et al., 2006, Does the expression of c-kit (CD117) in neuroendocrine tumors represent a target for therapy?, Ann. N. Y. Acad. Sci.
    Guida et al., 2007, Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants., Clin. Cancer Res.

  • CGI: KIT

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Quintás-Cardama et al., 2008, Complete response of stage IV anal mucosal melanoma expressing KIT Val560Asp to the multikinase inhibitor sorafenib., Nat Clin Pract Oncol
    Handolias et al., 2010, Clinical responses observed with imatinib or sorafenib in melanoma patients expressing mutations in KIT., Br. J. Cancer
    Wasag et al., 2011, Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis., Exp. Hematol.

  • DoCM: KIT

    • Version: 27-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Wasag et al., 2011, Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis., Exp. Hematol.
    Johnson et al., 2013, Hidden mastocytosis in acute myeloid leukemia with t(8;21)(q22;q22)., Am. J. Clin. Pathol.
    Gajiwala et al., 2009, KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients., Proc. Natl. Acad. Sci. U.S.A.

  • DTC: KIT

    • Version: 02-September-2020

    Alternate Names:

    Gene Info:

    Publications:
    Huang et al., 2010, Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant., J. Med. Chem.

  • ChemblInteractions: SCFR

    • Version: chembl_23

    Alternate Names:
    SCFR GENE_SYMBOL
    KIT GENE_SYMBOL
    Mast/stem cell growth factor receptor Kit UNIPROT

    Gene Info:

    Publications:

  • TALC: KIT

    • Version: 12-May-2016

    Alternate Names:
    KIT Gene Symbol

    Gene Info:

    Publications:

  • MyCancerGenome: KIT

    • Version: 20-Jun-2017

    Alternate Names:
    3815 Entrez Gene Id
    KIT MyCancerGenome Gene Symbol
    KIT MyCancerGenome Reported Gene Name

    Gene Info:

    Publications:

  • HingoraniCasas: ENSG00000157404

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000157404 Gene Symbol
    KIT Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • OncoKB: KIT

    • Version: 23-July-2020

    Alternate Names:
    3815 OncoKB Entrez Id
    PBT OncoKB Gene Synonym
    C-Kit OncoKB Gene Synonym

    Gene Info:

    Publications:

  • Pharos: KIT

    • Version: 03-September-2020

    Alternate Names:
    Mast/stem cell growth factor receptor Kit Gene Name
    P10721 UniProt ID

    Gene Info:

    Gene Categories:
    KINASE, TRANSCRIPTION FACTOR

    Publications:

  • GO: KIT

    • Version: 05-September-2020

    Alternate Names:
    SCFR GO Gene Synonym

    Gene Info:

    Gene Categories:
    TYROSINE KINASE, EXTERNAL SIDE OF PLASMA MEMBRANE

    Publications:

  • Tempus: KIT

    • Version: 11-November-2018

    Alternate Names:
    KIT Gene Symbol

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • dGene: KIT

    • Version: 27-Jun-2013

    Alternate Names:
    3815 Gene ID
    C-Kit dGene Synonym
    CD117 dGene Synonym

    Gene Info:

    Gene Categories:
    KINASE, TYROSINE KINASE

    Publications:

  • TTD: Tyrosine-protein kinase Kit

    • Version: 2020.06.01

    Alternate Names:
    KIT TTD Gene Abbreviation
    T57700 TTD Target ID

    Gene Info:

    Publications:

  • MyCancerGenomeClinicalTrial: KIT

    • Version: 30-February-2014

    Alternate Names:

    Gene Info:

    Publications:

  • MskImpact: KIT

    • Version: May-2015

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • ClearityFoundationClinicalTrial: KIT

    • Version: 15-June-2013

    Alternate Names:

    Gene Info:

    Publications:

  • FoundationOneGenes: KIT

    • Version: 03-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • CarisMolecularIntelligence: KIT

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • FDA: KIT

    • Version: 04-September-2020

    Alternate Names:

    Gene Info:

    Publications:

  • Oncomine: KIT

    • Version: v3

    Alternate Names:

    Gene Info:

    Gene Categories:
    CLINICALLY ACTIONABLE

    Publications:

  • COSMIC: KIT

    • Version: 4-Sep-2020

    Alternate Names:

    Gene Info:

    Gene Categories:
    DRUG RESISTANCE

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21