DGIdb - DASATINIB Drug Record

DASATINIB chembl:CHEMBL1421 ApprovedAntineoplasticImmunotherapy

Alternate Names:

SPRYCEL
DASATINIB
BMS-354825 HYDRATE
BMS-354825
DASATINIB HYDRATE
BMS-354825-03
DASATINIB MONOHYDRATE
BMS 345825
BMS 35482513
ANHYDROUS DASATINIB
BMS 354825
SPRYCEL®
ANH. DASATINIB
DASATINIB ANHYDROUS
DASATINIB (ANH.)
chemidplus:302962-49-8
drugbank:01254
pubchem.compound:3062316
chembl:CHEMBL1421
rxcui:1546019

Drug Info:

Year of Approval	2006
Drug Class	antineoplastic agents, protein kinase inhibitors
FDA Approval	Chronic myelogenous leukemia (Philadelphia chromosome positive), Acute lymphoblastic leukemia (Ph +)
Drug Class	Kinase Inhibitors
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antineoplastic agent
Source Reported Drug Name(s)	Dasatinib/Sprycel/ BMS-354825
Pharmaceutical Developer	Bristol-Myers Squibb
Source Reported Drug Name(s)	Dasatinib
Drug Class	Kit Inhibitor
Drug Categories	cytochrome p-450 cyp1a2 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 cyp3a5 substrates
Drug Categories	cytochrome p-450 cyp3a5 substrates with a narrow therapeutic index
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	drugs causing inadvertant photosensitivity
Drug Categories	kinase inhibitor
Drug Categories	p-glycoprotein inhibitors
Drug Categories	p-glycoprotein substrates
Drug Categories	p-glycoprotein substrates with narrow therapeutic index
Drug Categories	photosensitizing agents
Drug Categories	potential qtc-prolonging agents
Drug Categories	qtc prolonging agents
Drug Categories	tyrosine kinase inhibitors

(16 More Sources)

Publications:

Buettner et al., 2008, Inhibition of Src family kinases with dasatinib blocks migration and invasion of human melanoma cells., Mol. Cancer Res.
Konecny et al., 2009, Activity of the multikinase inhibitor dasatinib against ovarian cancer cells., Br. J. Cancer
Faoro et al., 2010, EphA2 mutation in lung squamous cell carcinoma promotes increased cell survival, cell invasion, focal adhesions, and mammalian target of rapamycin activation., J. Biol. Chem.
Lindauer et al., 2010, Dasatinib., Recent Results Cancer Res.
Wang et al., 2007, Identification of candidate predictive and surrogate molecular markers for dasatinib in prostate cancer: rationale for patient selection and efficacy monitoring., Genome Biol.
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
Roberts et al., 2014, Targetable kinase-activating lesions in Ph-like acute lymphoblastic leukemia., N. Engl. J. Med.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Al-Ali et al., 2004, High incidence of BCR-ABL kinase domain mutations and absence of mutations of the PDGFR and KIT activation loops in CML patients with secondary resistance to imatinib., Hematol. J.
An et al., 2010, BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: a review., Leuk. Res.
O'Hare et al., 2004, Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML., Blood
Testoni et al., 2016, Somatically mutated ABL1 is an actionable and essential NSCLC survival gene., EMBO Mol Med
Chahardouli et al., 2013, Detection of BCR-ABL kinase domain mutations in patients with chronic myeloid leukemia on imatinib., Hematology
Burgess MR et al., 2005, Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance., Proc Natl Acad Sci U S A
Müller MC et al., 2009, Dasatinib treatment of chronic-phase chronic myeloid leukemia: analysis of responses according to preexisting BCR-ABL mutations., Blood
von Bubnoff et al., 2002, BCR-ABL gene mutations in relation to clinical resistance of Philadelphia-chromosome-positive leukaemia to STI571: a prospective study., Lancet
Qin et al., 2011, Characteristics of BCR-ABL kinase domain point mutations in Chinese imatinib-resistant chronic myeloid leukemia patients., Ann. Hematol.
Talpaz M et al., 2006, Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias., N Engl J Med
Tomita O et al., 2014, Sensitivity of SNX2-ABL1 toward tyrosine kinase inhibitors distinct from that of BCR-ABL1., Leuk Res
Doi et al., 2009, High-resolution melting analysis for a reliable and two-step scanning of mutations in the tyrosine kinase domain of the chimerical bcr-abl gene., Int. J. Hematol.
Deguchi Y et al., 2008, Comparison of imatinib, dasatinib, nilotinib and INNO-406 in imatinib-resistant cell lines., Leuk Res
Pemovska T et al., 2015, Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation., Nature
Sharma et al., 2010, Mutations in ABL kinase domain are associated with inferior progression-free survival., Leuk. Lymphoma
Piccaluga et al., 2007, Tyrosine kinase inhibitors for the treatment of Philadelphia chromosome-positive adult acute lymphoblastic leukemia., Cancer
Sorel et al., 2004, Evidence of ABL-kinase domain mutations in highly purified primitive stem cell populations of patients with chronic myelogenous leukemia., Biochem. Biophys. Res. Commun.
Strhakova et al., 2011, Use of direct sequencing for detection of mutations in the BCR-ABL kinase domain in Slovak patients with chronic myeloid leukemia., Neoplasma
Jabbour et al., 2008, Characteristics and outcome of chronic myeloid leukemia patients with F317L BCR-ABL kinase domain mutation after therapy with tyrosine kinase inhibitors., Blood
Branford et al., 2002, High frequency of point mutations clustered within the adenosine triphosphate-binding region of BCR/ABL in patients with chronic myeloid leukemia or Ph-positive acute lymphoblastic leukemia who develop imatinib (STI571) resistance., Blood
Elias et al., 2014, BCR-ABL kinase domain mutations, including 2 novel mutations in imatinib resistant Malaysian chronic myeloid leukemia patients-Frequency and clinical outcome., Leuk. Res.
Jones et al., 2008, Kinase domain point mutations in Philadelphia chromosome-positive acute lymphoblastic leukemia emerge after therapy with BCR-ABL kinase inhibitors., Cancer
MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
von Bubnoff et al., 2003, Inhibition of wild-type and mutant Bcr-Abl by pyrido-pyrimidine-type small molecule kinase inhibitors., Cancer Res.
Soverini et al., 2011, BCR-ABL kinase domain mutation analysis in chronic myeloid leukemia patients treated with tyrosine kinase inhibitors: recommendations from an expert panel on behalf of European LeukemiaNet., Blood
Eide et al., 2011, The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile., Cancer Res.
Hughes et al., 2009, Impact of baseline BCR-ABL mutations on response to nilotinib in patients with chronic myeloid leukemia in chronic phase., J. Clin. Oncol.
Bradeen HA et al., 2006, Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)-based mutagenesis screen: high efficacy of drug combinations., Blood
Hochhaus et al., 2002, Molecular and chromosomal mechanisms of resistance to imatinib (STI571) therapy., Leukemia
Hammerman et al., 2011, Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer., Cancer Discov
Pitini et al., 2013, Response to dasatinib in a patient with SQCC of the lung harboring a discoid-receptor-2 and synchronous chronic myelogenous leukemia., Lung Cancer
Day et al., 2008, Inhibition of collagen-induced discoidin domain receptor 1 and 2 activation by imatinib, nilotinib and dasatinib., Eur. J. Pharmacol.
Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.
Koschmann C et al., 2016, Characterizing and targeting PDGFRA alterations in pediatric high-grade glioma., Oncotarget
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
Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.
Prenen et al., 2006, Efficacy of the kinase inhibitor SU11248 against gastrointestinal stromal tumor mutants refractory to imatinib mesylate., Clin. Cancer Res.
Lasota et al., 2004, A great majority of GISTs with PDGFRA mutations represent gastric tumors of low or no malignant potential., Lab. Invest.
Hirota et al., 2003, Gain-of-function mutations of platelet-derived growth factor receptor alpha gene in gastrointestinal stromal tumors., Gastroenterology
Yoo et al., 2016, Efficacy of Imatinib in Patients with Platelet-Derived Growth Factor Receptor Alpha-Mutated Gastrointestinal Stromal Tumors., Cancer Res Treat
Heinrich et al., 2003, Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor., J. Clin. Oncol.
Heinrich et al., 2006, Molecular correlates of imatinib resistance in gastrointestinal stromal tumors., J. Clin. Oncol.
Dewaele et al., 2008, Activity of dasatinib, a dual SRC/ABL kinase inhibitor, and IPI-504, a heat shock protein 90 inhibitor, against gastrointestinal stromal tumor-associated PDGFRAD842V mutation., Clin. Cancer Res.
Heinrich et al., 2012, Crenolanib inhibits the drug-resistant PDGFRA D842V mutation associated with imatinib-resistant gastrointestinal stromal tumors., Clin. Cancer Res.
Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
Paik et al., 2011, Clinical characteristics of patients with lung adenocarcinomas harboring BRAF mutations., J. Clin. Oncol.
Pratilas et al., 2008, Genetic predictors of MEK dependence in non-small cell lung cancer., Cancer Res.
Cardarella et al., 2013, Clinical, pathologic, and biologic features associated with BRAF mutations in non-small cell lung cancer., Clin. Cancer Res.
Gandhi et al., 2009, Alterations in genes of the EGFR signaling pathway and their relationship to EGFR tyrosine kinase inhibitor sensitivity in lung cancer cell lines., PLoS ONE
Bardelli et al., 2012, The road to resistance: EGFR mutation and cetuximab., Nat. Med.
Girotti et al., 2013, Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma., Cancer Discov
De Roock et al., 2009, Clinical biomarkers in oncology: focus on colorectal cancer., Mol Diagn Ther
Bentivegna et al., 2008, Rapid identification of somatic mutations in colorectal and breast cancer tissues using mismatch repair detection (MRD)., Hum. Mutat.
Davies et al., 2002, Mutations of the BRAF gene in human cancer., Nature
Beadnell et al., 2016, The Mitogen-Activated Protein Kinase Pathway Facilitates Resistance to the Src Inhibitor Dasatinib in Thyroid Cancer., Mol. Cancer Ther.
Sen et al., 2012, Kinase-impaired BRAF mutations in lung cancer confer sensitivity to dasatinib., Sci Transl Med
Naoki et al., 2002, Missense mutations of the BRAF gene in human lung adenocarcinoma., Cancer Res.
Brose et al., 2002, BRAF and RAS mutations in human lung cancer and melanoma., Cancer Res.
Tejpar et al., 2010, Prognostic and predictive biomarkers in resected colon cancer: current status and future perspectives for integrating genomics into biomarker discovery., Oncologist
Rizzo et al., 2010, Prognostic vs predictive molecular biomarkers in colorectal cancer: is KRAS and BRAF wild type status required for anti-EGFR therapy?, Cancer Treat. Rev.
Saha et al., 2016, Isocitrate Dehydrogenase Mutations Confer Dasatinib Hypersensitivity and SRC Dependence in Intrahepatic Cholangiocarcinoma., Cancer Discov
Kamath et al., 2008, Preclinical pharmacokinetics and in vitro metabolism of dasatinib (BMS-354825): a potent oral multi-targeted kinase inhibitor against SRC and BCR-ABL., Cancer Chemother. Pharmacol.
Nam et al., 2005, Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells., Cancer Res.
Du et al., 2009, Bead-based profiling of tyrosine kinase phosphorylation identifies SRC as a potential target for glioblastoma therapy., Nat. Biotechnol.
Getlik M et al., 2009, Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc., J Med Chem
Quintás-Cardama et al., 2006, Targeting ABL and SRC kinases in chronic myeloid leukemia: experience with dasatinib., Future Oncol
Gilani et al., 2016, UM-164: A Potent c-Src/p38 Kinase Inhibitor with In Vivo Activity against Triple-Negative Breast Cancer., Clin. Cancer Res.
Zhang CH et al., 2015, Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer., J Med Chem
Serrels et al., 2006, Identification of potential biomarkers for measuring inhibition of Src kinase activity in colon cancer cells following treatment with dasatinib., Mol. Cancer Ther.
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.
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
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
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.
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
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.
Nam et al., 2007, Dasatinib (BMS-354825) inhibits Stat5 signaling associated with apoptosis in chronic myelogenous leukemia cells., Mol. Cancer Ther.
Fiskus et al., 2006, Cotreatment with vorinostat (suberoylanilide hydroxamic acid) enhances activity of dasatinib (BMS-354825) against imatinib mesylate-sensitive or imatinib mesylate-resistant chronic myelogenous leukemia cells., Clin. Cancer Res.
Ishibashi T et al., 2016, Ph-like ALL-related novel fusion kinase ATF7IP-PDGFRB exhibits high sensitivity to tyrosine kinase inhibitors in murine cells., Exp Hematol
Zhang G et al., 2017, Acute Lymphoblastic Leukemia Patient with Variant ATF7IP/PDGFRB Fusion and Favorable Response to Tyrosine Kinase Inhibitor Treatment: A Case Report., Am J Case Rep
Zhang et al., 2006, New assignments for multitasking signal transduction inhibitors., Mol. Pharmacol.
Chen et al., 2006, Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib)., Mol. Pharmacol.
Kneidinger M et al., 2008, The effects of dasatinib on IgE receptor-dependent activation and histamine release in human basophils., Blood
Javadi et al., 2013, CBL linker region and RING finger mutations lead to enhanced granulocyte-macrophage colony-stimulating factor (GM-CSF) signaling via elevated levels of JAK2 and LYN., J. Biol. Chem.
Margutti et al., 2007, Are MAP kinases drug targets? Yes, but difficult ones., ChemMedChem
Trevino et al., 2006, Inhibition of SRC expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model., Am. J. Pathol.
Shen et al., 2015, c-Myc alterations confer therapeutic response and acquired resistance to c-Met inhibitors in MET-addicted cancers., Cancer Res.
Ambrogio et al., 2016, Combined inhibition of DDR1 and Notch signaling is a therapeutic strategy for KRAS-driven lung adenocarcinoma., Nat. Med.
Das et al., 2006, 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor., J. Med. Chem.
Shah NP et al., 2004, Overriding imatinib resistance with a novel ABL kinase inhibitor., Science
Nautiyal et al., 2011, Curcumin enhances dasatinib-induced inhibition of growth and transformation of colon cancer cells., Int. J. Cancer
Parseghian et al., 2017, Dual Inhibition of EGFR and c-Src by Cetuximab and Dasatinib Combined with FOLFOX Chemotherapy in Patients with Metastatic Colorectal Cancer., Clin. Cancer Res.
Dunn et al., 2011, Dasatinib sensitizes KRAS mutant colorectal tumors to cetuximab., Oncogene
Hayes et al., 2016, Long-Term ERK Inhibition in KRAS-Mutant Pancreatic Cancer Is Associated with MYC Degradation and Senescence-like Growth Suppression., Cancer Cell
Ichihara et al., 2017, SFK/FAK Signaling Attenuates Osimertinib Efficacy in Both Drug-Sensitive and Drug-Resistant Models of EGFR-Mutant Lung Cancer., Cancer Res.
Skoglund K et al., 2014, Single-nucleotide polymorphisms of ABCG2 increase the efficacy of tyrosine kinase inhibitors in the K562 chronic myeloid leukemia cell line., Pharmacogenet Genomics
Hantschel O et al., 2007, The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib., Proc Natl Acad Sci U S A
Miller et al., 2016, Synthetic Lethal Targeting of ARID1A-Mutant Ovarian Clear Cell Tumors with Dasatinib., Mol. Cancer Ther.
Natsume H et al., 2012, The CRKL gene encoding an adaptor protein is amplified, overexpressed, and a possible therapeutic target in gastric cancer., J Transl Med

DASATINIB NR4A3

Interaction Score: 1.42

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17684099

Sources:
DrugBank
DASATINIB STAT5B

Interaction Score: 1.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name dasatinib, BMS-354825,Sprycel

Novel drug target Established target

PMIDs:
17431118 17020995

Sources:
TEND TdgClinicalTrial DrugBank
DASATINIB CRKL

Interaction Score: 0.71

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
22591714

Sources:
CIViC
DASATINIB ABL2

Interaction Score: 0.63

Interaction Types & Directionality:

multitarget

Interaction Info:

Trial Name dasatinib, BMS-354825,Sprycel

Novel drug target Established target

PMIDs:
20072833 25207766 11752352 17016423

Sources:
TEND TdgClinicalTrial CIViC DrugBank
DASATINIB EPHA2

Interaction Score: 0.56

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
19010823 19861960 20360610 20072833 18047674 17139284 17016423

Sources:
MyCancerGenomeClinicalTrial TEND DTC DoCM TdgClinicalTrial DrugBank ChemblInteractions CGI
DASATINIB DDR2

Interaction Score: 0.55

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family BCR-ABL inhibitor 2nd gen

Alteration DDR2:S768R

Alteration DDR2:I638F,L239R,G253C,G774V,L63V,G505S

PMIDs:
22328973 23932362 18938156

Sources:
MyCancerGenomeClinicalTrial DoCM CIViC CGI
DASATINIB ABL1

Interaction Score: 0.44

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

combination therapy [Nilotinib,Dasatinib]

Drug family [BCR-ABL inhibitor 2nd gen]

Alteration ABL1:T315I

PMIDs:
14745431 20537386 15256422 26758680 23676790 15705718 19779040 11853795 20697894 16775234 24367893 19466505 18191450 25686603 20367437 17701954 25207766 15381060 21895409 18818391 11964322 11752352 24456693 18615627 25157968 14559829 17016423 21562040 21505103 19652056 16772610 12399961

Sources:
TEND OncoKB FDA PharmGKB DoCM JAX-CKB TdgClinicalTrial CIViC DrugBank COSMIC MyCancerGenome GuideToPharmacology ChemblInteractions CGI
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
DASATINIB ABI1

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
DASATINIB IDH2

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type intrahepatic cholangiocarcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
27231123

Sources:
JAX-CKB CGI
DASATINIB CBL

Interaction Score: 0.36

Interaction Types & Directionality:

n/a

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status preclinical

PMIDs:
23696637

Sources:
DoCM CGI
DASATINIB BCR

Interaction Score: 0.3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes Targets BCR-ABL fusion protein

Fusion protein BCR:ABL1

PMIDs:
15256671

Sources:
FDA PharmGKB DrugBank TALC
DASATINIB EPHA5

Interaction Score: 0.28

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18180381

Sources:
DrugBank
DASATINIB PPAT

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18180381

Sources:
DrugBank
DASATINIB ARID1A

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
27364904

Sources:
CIViC
DASATINIB TEC

Interaction Score: 0.24

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17684099

Sources:
DTC
DASATINIB SIK3

Interaction Score: 0.24

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
DASATINIB FGR

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
18180381

Sources:
DrugBank ChemblInteractions
DASATINIB PDGFRA

Interaction Score: 0.21

Interaction Types & Directionality:

n/a

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status preclinical

PMIDs:
22328973 15928335 27582545 15685537 22718859 16638875 15146165 12949711 26130666 25157968 14645423 16954519 18794084 22745105

Sources:
DTC OncoKB DoCM JAX-CKB CIViC CGI
DASATINIB CSK

Interaction Score: 0.2

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18180381

Sources:
DrugBank
DASATINIB SIK1

Interaction Score: 0.18

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology
DASATINIB FYN

Interaction Score: 0.16

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name dasatinib, BMS-354825,Sprycel

Mechanism of Interaction SRC inhibitor

PMIDs:
20072833 11752352 17139284 17016423

Sources:
TEND TdgClinicalTrial TTD DrugBank ChemblInteractions
DASATINIB SRC

Interaction Score: 0.16

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction SRC inhibitor

Novel drug target Established target

PMIDs:
27231123 17429625 16230377 19098899 19462975 17155893 27154914 27222538 25835317 11752352 17148760 16397263

Sources:
CancerCommons TEND DTC JAX-CKB TdgClinicalTrial TTD DrugBank TALC GuideToPharmacology ChemblInteractions
DASATINIB SRMS

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions
DASATINIB BRAF

Interaction Score: 0.15

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Variant Effect reduced kinase activity

Pathway activation

PMIDs:
26619011 21483012 19010912 23833300 19238210 22310681 23242808 19537845 18186519 12068308 27222538 22649091 25157968 12460919 12460918 20350999 21129611

Sources:
MyCancerGenomeClinicalTrial DoCM JAX-CKB CGI
DASATINIB SIK2

Interaction Score: 0.13

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
DASATINIB MAP3K20

Interaction Score: 0.13

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18180381

Sources:
DTC DrugBank
DASATINIB FES

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB EPHB4

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18180381

Sources:
DrugBank
DASATINIB MAP3K10

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB PDGFRB

Interaction Score: 0.1

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Platelet-derived growth factor receptor beta inhibitor

Trial Name dasatinib, BMS-354825,Sprycel

PMIDs:
26703895 20072833 29133777 16497876 16436588

Sources:
MyCancerGenomeClinicalTrial TEND DTC TdgClinicalTrial CIViC DrugBank ChemblInteractions
DASATINIB LCK

Interaction Score: 0.08

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

Trial Name dasatinib, BMS-354825,Sprycel

Novel drug target Established target

Mechanism of Interaction SRC inhibitor

PMIDs:
17154512 20072833 11752352

Sources:
TEND TdgClinicalTrial TTD DrugBank ChemblInteractions
DASATINIB HSPA8

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18180381

Sources:
DrugBank
DASATINIB CDC42BPA

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB APC

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
20473900

Sources:
JAX-CKB
DASATINIB CSF3R

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family BCR-ABL inhibitor 2nd gen

Alteration CSF3R:Q741.,Y752.,W791.,T615A,T618I

PMIDs:
None found

Sources:
CGI
DASATINIB PTK6

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB FRK

Interaction Score: 0.07

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
18180381

Sources:
DrugBank ChemblInteractions
DASATINIB DYRK3

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB HCK

Interaction Score: 0.06

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
DTC ChemblInteractions
DASATINIB BTK

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
17684099

Sources:
DTC DrugBank
DASATINIB LYN

Interaction Score: 0.05

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
18180381

Sources:
DrugBank ChemblInteractions
DASATINIB KRAS

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dasatinib + Demcizumab

Indication/Tumor Type lung adenocarcinoma

Response Type sensitive

PMIDs:
26855149 27231123 28280091 27222538 20956938 26725216

Sources:
JAX-CKB CIViC
DASATINIB HRAS

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Approval Status Preclinical - Cell line xenograft

Response Type resistant

combination therapy Dasatinib + SCH772984

PMIDs:
27222538

Sources:
JAX-CKB
DASATINIB IRAK4

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB PKN2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB NF1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

Drug family BCR-ABL inhibitor 2nd gen

Alteration NF1:del

Alteration NF1:.

PMIDs:
None found

Sources:
CGI
DASATINIB ACVR1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB TNK2

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB LIMK1

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB YES1

Interaction Score: 0.03

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name dasatinib, BMS-354825,Sprycel

Novel drug target Established target

Mechanism of Interaction SRC inhibitor

PMIDs:
17541990 20072833 16507911

Sources:
TEND DTC TdgClinicalTrial DrugBank ChemblInteractions
DASATINIB AXL

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB PLK4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB MINK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB TAOK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB ABCG2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24322003

Sources:
PharmGKB
DASATINIB SLK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB MAP4K5

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB SYK

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB MAPK14

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18180381

Sources:
DTC DrugBank
DASATINIB BLK

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction SRC inhibitor

PMIDs:
None found

Sources:
ChemblInteractions
DASATINIB ERBB4

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB MAP2K2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB MAP2K1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB MET

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type non-small cell lung carcinoma

Response Type predicted – sensitive

Approval Status Preclinical - Cell culture

PMIDs:
26483207

Sources:
JAX-CKB
DASATINIB AURKB

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB FGFR3

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB CSF1R

Interaction Score: 0.01

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes

PMIDs:
None found

Sources:
TALC
DASATINIB PIK3CA

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dasatinib + Demcizumab

Indication/Tumor Type lung adenocarcinoma

Response Type sensitive

PMIDs:
26855149

Sources:
JAX-CKB
DASATINIB JAK2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB EGFR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dasatinib + Osimertinib

Indication/Tumor Type lung cancer

Response Type sensitive

PMIDs:
28416483

Sources:
JAX-CKB
DASATINIB FGFR1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB IDH1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type chondrosarcoma

Response Type resistant

Approval Status Preclinical

PMIDs:
27231123

Sources:
JAX-CKB CIViC CGI
DASATINIB PPARD

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB KDR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB ERBB2

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB TP53

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

combination therapy Dasatinib + Demcizumab

Indication/Tumor Type lung adenocarcinoma

Response Type sensitive

PMIDs:
26855149

Sources:
JAX-CKB
DASATINIB SMAD3

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB GMNN

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
DASATINIB AR

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DrugBank: DB01254

Version: 5.1.7

Alternate Names:

302962-49-8 CAS Number

Apo-dasatinib Drug Brand

Sprycel Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Shah NP et al., 2004, Overriding imatinib resistance with a novel ABL kinase inhibitor., Science

Das et al., 2006, 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor., J. Med. Chem.

Lindauer et al., 2010, Dasatinib., Recent Results Cancer Res.

CancerCommons: DASATINIB
- Version: 25-July-2013
Alternate Names:

3062316 PubChem Drug ID

Sprycel Drug Trade Name

Sprycel Drug Development Name

Drug Info:

Drug Class Kit Inhibitor

Source Reported Drug Name(s) Dasatinib

Pharmaceutical Developer Bristol-Myers Squibb

Publications:
MyCancerGenome: DASATINIB
- Version: 20-Jun-2017
Alternate Names:

BMS-354825 Development Name

SPRYCEL Trade Name

Drug Info:

Drug Class Kinase Inhibitors

FDA Approval Chronic myelogenous leukemia (Philadelphia chromosome positive), Acute lymphoblastic leukemia (Ph +)

Publications:
TdgClinicalTrial: DASATINIB
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antineoplastic agent

Drug Class Small Molecule

FDA Approval approved

Publications:
TEND: DASATINIB
- Version: 01-August-2011
Alternate Names:

Drug Info:

Drug Class antineoplastic agents, protein kinase inhibitors

Year of Approval 2006

Publications:

DTC: DASATINIB

Version: 02-September-2020

Alternate Names:

CHEMBL1421 ChEMBL Drug ID

Drug Info:

Publications:

Getlik M et al., 2009, Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc., J Med Chem

Zhang CH et al., 2015, Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer., J Med Chem

Hantschel O et al., 2007, The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib., Proc Natl Acad Sci U S A

JAX-CKB: Dasatinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Saha et al., 2016, Isocitrate Dehydrogenase Mutations Confer Dasatinib Hypersensitivity and SRC Dependence in Intrahepatic Cholangiocarcinoma., Cancer Discov

Wasag et al., 2011, Novel, activating KIT-N822I mutation in familial cutaneous mastocytosis., Exp. Hematol.

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

CGI: Dasatinib

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Buettner et al., 2008, Inhibition of Src family kinases with dasatinib blocks migration and invasion of human melanoma cells., Mol. Cancer Res.

Konecny et al., 2009, Activity of the multikinase inhibitor dasatinib against ovarian cancer cells., Br. J. Cancer

Wang et al., 2007, Identification of candidate predictive and surrogate molecular markers for dasatinib in prostate cancer: rationale for patient selection and efficacy monitoring., Genome Biol.

PharmGKB: dasatinib
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Skoglund K et al., 2014, Single-nucleotide polymorphisms of ABCG2 increase the efficacy of tyrosine kinase inhibitors in the K562 chronic myeloid leukemia cell line., Pharmacogenet Genomics

DoCM: DASATINIB

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Corless et al., 2005, PDGFRA mutations in gastrointestinal stromal tumors: frequency, spectrum and in vitro sensitivity to imatinib., J. Clin. Oncol.

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

Cassier et al., 2012, Outcome of patients with platelet-derived growth factor receptor alpha-mutated gastrointestinal stromal tumors in the tyrosine kinase inhibitor era., Clin. Cancer Res.

CIViC: DASATINIB

Version: 14-September-2020

Alternate Names:

Drug Info:

Publications:

An et al., 2010, BCR-ABL tyrosine kinase inhibitors in the treatment of Philadelphia chromosome positive chronic myeloid leukemia: a review., Leuk. Res.

Testoni et al., 2016, Somatically mutated ABL1 is an actionable and essential NSCLC survival gene., EMBO Mol Med

Burgess MR et al., 2005, Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance., Proc Natl Acad Sci U S A

TALC: DASATINIB
- Version: 12-May-2016
Alternate Names:

SPRYCEL Drug Trade Name

BMS-354825 Drug Synonym

Drug Info:

Publications:
TTD: Dasatinib
- Version: 2020.06.01
Alternate Names:

D0E6XR TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1421
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
GuideToPharmacology: 178102305
- Version: 29-September-2020
Alternate Names:

Drug Info:

Publications:
MyCancerGenomeClinicalTrial: DASATINIB
- Version: 30-February-2014
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1421
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:
OncoKB: Dasatinib
- Version: 23-July-2020
Alternate Names:

Drug Info:

Publications:
FDA: Dasatinib
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:
COSMIC: Dasatinib
- Version: 4-Sep-2020
Alternate Names:

Drug Info:

Publications:

Trial Name	dasatinib, BMS-354825,Sprycel
Novel drug target	Established target

Clinical Status	preclinical
Pathway	activation
Variant Effect	gain-of-function

Drug family	BCR-ABL inhibitor 2nd gen
Alteration	DDR2:S768R
Alteration	DDR2:I638F,L239R,G253C,G774V,L63V,G505S

combination therapy	[Nilotinib,Dasatinib]
Drug family	[BCR-ABL inhibitor 2nd gen]
Alteration	ABL1:T315I

Reported Cancer Type	Melanoma
Clinical Status	preclinical
Clinical Status	early trials

Indication/Tumor Type	intrahepatic cholangiocarcinoma
Response Type	sensitive
Approval Status	Preclinical

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

Direct Interaction	yes
Mechanism of Interaction	SRC inhibitor
Novel drug target	Established target

Direct Interaction	yes
Mechanism of Interaction	Platelet-derived growth factor receptor beta inhibitor
Trial Name	dasatinib, BMS-354825,Sprycel

Indication/Tumor Type	colorectal cancer
Response Type	sensitive
Approval Status	Preclinical

antagonist (inhibitory)
inhibitor (inhibitory)

multitarget
inhibitor (inhibitory)

antagonist (inhibitory)
inhibitor (inhibitory)

combination therapy	Dasatinib + Demcizumab
Indication/Tumor Type	lung adenocarcinoma
Response Type	sensitive

Approval Status	Preclinical - Cell line xenograft
Response Type	resistant
combination therapy	Dasatinib + SCH772984

Indication/Tumor Type	non-small cell lung carcinoma
Response Type	predicted – sensitive
Approval Status	Preclinical - Cell culture

combination therapy	Dasatinib + Osimertinib
Indication/Tumor Type	lung cancer
Response Type	sensitive

Indication/Tumor Type	chondrosarcoma
Response Type	resistant
Approval Status	Preclinical

302962-49-8	CAS Number
Apo-dasatinib	Drug Brand
Sprycel	Drug Brand

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

3062316	PubChem Drug ID
Sprycel	Drug Trade Name
Sprycel	Drug Development Name

DASATINIB Drug Record

DASATINIB chembl:CHEMBL1421 ApprovedAntineoplasticImmunotherapy

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17684099

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name dasatinib, BMS-354825,Sprycel Novel drug target Established target

PMIDs: 17431118 17020995

Sources: TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 22591714

Sources: CIViC

Interaction Types & Directionality: multitarget

Interaction Info: Trial Name dasatinib, BMS-354825,Sprycel Novel drug target Established target

PMIDs: 20072833 25207766 11752352 17016423

Sources: TEND TdgClinicalTrial CIViC DrugBank

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

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

PMIDs: 19010823 19861960 20360610 20072833 18047674 17139284 17016423

Sources: MyCancerGenomeClinicalTrial TEND DTC DoCM TdgClinicalTrial DrugBank ChemblInteractions CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Drug family BCR-ABL inhibitor 2nd gen Alteration DDR2:S768R Alteration DDR2:I638F,L239R,G253C,G774V,L63V,G505S

PMIDs: 22328973 23932362 18938156

Sources: MyCancerGenomeClinicalTrial DoCM CIViC CGI

Interaction Types & Directionality: multitarget inhibitor (inhibitory)

Interaction Info: combination therapy [Nilotinib,Dasatinib] Drug family [BCR-ABL inhibitor 2nd gen] Alteration ABL1:T315I

PMIDs: 14745431 20537386 15256422 26758680 23676790 15705718 19779040 11853795 20697894 16775234 24367893 19466505 18191450 25686603 20367437 17701954 25207766 15381060 21895409 18818391 11964322 11752352 24456693 18615627 25157968 14559829 17016423 21562040 21505103 19652056 16772610 12399961

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

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

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type intrahepatic cholangiocarcinoma Response Type sensitive Approval Status Preclinical

PMIDs: 27231123

Sources: JAX-CKB CGI

Interaction Types & Directionality: n/a

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

PMIDs: 23696637

Sources: DoCM CGI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Notes Targets BCR-ABL fusion protein Fusion protein BCR:ABL1

PMIDs: 15256671

Sources: FDA PharmGKB DrugBank TALC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18180381

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18180381

Sources: DrugBank

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 27364904

Sources: CIViC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 17684099

Sources: DTC

Interaction Types & Directionality: inhibitor (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction SRC inhibitor Direct Interaction yes

PMIDs: 18180381

Sources: DrugBank ChemblInteractions

Interaction Types & Directionality: n/a

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

PMIDs: 22328973 15928335 27582545 15685537 22718859 16638875 15146165 12949711 26130666 25157968 14645423 16954519 18794084 22745105

Interaction Types & Directionality:

n/a

PMIDs:
17684099

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name dasatinib, BMS-354825,Sprycel

Novel drug target Established target

PMIDs:
17431118 17020995

Sources:
TEND TdgClinicalTrial DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
22591714

Sources:
CIViC

Interaction Types & Directionality:

multitarget

Interaction Info:

Trial Name dasatinib, BMS-354825,Sprycel

Novel drug target Established target

PMIDs:
20072833 25207766 11752352 17016423

Sources:
TEND TdgClinicalTrial CIViC DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Clinical Status preclinical

Pathway activation

Variant Effect gain-of-function

PMIDs:
19010823 19861960 20360610 20072833 18047674 17139284 17016423

Sources:
MyCancerGenomeClinicalTrial TEND DTC DoCM TdgClinicalTrial DrugBank ChemblInteractions CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Drug family BCR-ABL inhibitor 2nd gen

Alteration DDR2:S768R

Alteration DDR2:I638F,L239R,G253C,G774V,L63V,G505S

PMIDs:
22328973 23932362 18938156

Sources:
MyCancerGenomeClinicalTrial DoCM CIViC CGI

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

combination therapy [Nilotinib,Dasatinib]

Drug family [BCR-ABL inhibitor 2nd gen]

Alteration ABL1:T315I

PMIDs:
14745431 20537386 15256422 26758680 23676790 15705718 19779040 11853795 20697894 16775234 24367893 19466505 18191450 25686603 20367437 17701954 25207766 15381060 21895409 18818391 11964322 11752352 24456693 18615627 25157968 14559829 17016423 21562040 21505103 19652056 16772610 12399961

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

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

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type intrahepatic cholangiocarcinoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
27231123

Sources:
JAX-CKB CGI

Interaction Types & Directionality:

n/a

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status preclinical

PMIDs:
23696637

Sources:
DoCM CGI

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Notes Targets BCR-ABL fusion protein

Fusion protein BCR:ABL1

PMIDs:
15256671

Sources:
FDA PharmGKB DrugBank TALC

Interaction Types & Directionality:

n/a

PMIDs:
18180381

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
18180381

Sources:
DrugBank

Interaction Types & Directionality:

n/a

PMIDs:
27364904

Sources:
CIViC

Interaction Types & Directionality:

n/a

PMIDs:
17684099

Sources:
DTC

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction SRC inhibitor

Direct Interaction yes

PMIDs:
18180381

Sources:
DrugBank ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Variant Effect gain-of-function

Pathway activation

Clinical Status preclinical

PMIDs:
22328973 15928335 27582545 15685537 22718859 16638875 15146165 12949711 26130666 25157968 14645423 16954519 18794084 22745105

Sources:
DTC OncoKB DoCM JAX-CKB CIViC CGI

Interaction Types & Directionality:

n/a

PMIDs:
18180381

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Inhibition

Endogenous Drug? False

Direct Interaction? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

multitarget

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name dasatinib, BMS-354825,Sprycel

Mechanism of Interaction SRC inhibitor

PMIDs:
20072833 11752352 17139284 17016423

Sources:
TEND TdgClinicalTrial TTD DrugBank ChemblInteractions