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 |
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 |
KINASE |
TYROSINE KINASE |
DRUG RESISTANCE |
EXTERNAL SIDE OF PLASMA MEMBRANE |
DRUGGABLE GENOME |
CLINICALLY ACTIONABLE |
TRANSCRIPTION FACTOR |
inhibitor (inhibitory) |
Pathway | activation |
Clinical Status | preclinical |
Variant Effect | gain-of-function |
antagonist (inhibitory) |
inhibitor (inhibitory) |
Reported Cancer Type | Melanoma |
Indication/Tumor Type | melanoma |
Response Type | sensitive |
multitarget |
antagonist (inhibitory) |
inhibitor (inhibitory) |
Approval Status | Guideline |
Indication/Tumor Type | prostate neuroendocrine neoplasm |
Approval Status | Phase II |
inhibitor (inhibitory) |
Alteration | KIT:449-514,550-592,627-664,664-714,788-828 |
Alteration | KIT:788-828 |
Alteration | KIT:Y553N |
inhibitor (inhibitory) |
Trial Name | MP-470 |
Novel drug target | Established target |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
inhibitor (inhibitory) |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Direct Interaction | yes |
Notes |
inhibitor (inhibitory) |
Indication/Tumor Type | gastrointestinal stromal tumor |
Response Type | sensitive |
Approval Status | Preclinical - Cell line xenograft |
inhibitor (inhibitory) |
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 |
inhibitor (inhibitory) |
Drug family | BCR-ABL inhibitor 3rd gen&Pan-TK inhibitor |
Alteration | KIT:788-828,829-860,550-592 |
Alteration | KIT:A829P,V654A,T670I |
inhibitor (inhibitory) |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Direct Interaction | yes |
Notes |
inhibitor (inhibitory) |
Direct Interaction? | True |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
antagonist (inhibitory) |
inhibitor (inhibitory) |
Reported Cancer Type | Melanoma |
Clinical Status | preclinical |
Clinical Status | early trials |
inhibitor (inhibitory) |
Response Type | decreased response |
Approval Status | Preclinical - Cell culture |
Approval Status | Phase II |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | True |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | True |
antagonist (inhibitory) |
inhibitor (inhibitory) |
Indication/Tumor Type | mast-cell leukemia |
Response Type | predicted – sensitive |
Approval Status | Preclinical - Patient cell culture |
inhibitor (inhibitory) |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Direct Interaction | yes |
Specific Action of the Ligand | Inhibition |
antagonist (inhibitory) |
inhibitor (inhibitory) |
Drug family | Pan-TK inhibitor |
Alteration | KIT:550-592,627-664,788-828,829-860 |
Alteration | KIT:D820E |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
Direct Interaction? | False |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Indication/Tumor Type | gastrointestinal stromal tumor |
Response Type | sensitive |
Approval Status | Preclinical |
inhibitor (inhibitory) |
Trial Name | vatalanib, PTK 787 |
Novel drug target | Established target |
Trial Name | Vatalanib |
inhibitor (inhibitory) |
Trial Name | axitinib, AG-013736 |
Novel drug target | Established target |
Reported Cancer Type | Prostate |
inhibitor (inhibitory) |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Details of the Assay for Interaction | Assay used apatinib mesylate (YN968D1) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Direct Interaction | yes |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Direct Interaction? | True |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Trial Name | E7080 |
Novel drug target | Established target |
inhibitor (inhibitory) |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
Notes | |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
inhibitor (inhibitory) |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
Direct Interaction | yes |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Novel drug target | Established target |
inhibitor (inhibitory) |
Details of the Assay for Interaction | In a biochemical enzyme activity assay. |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
inhibitor (inhibitory) |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Direct Interaction | yes |
inhibitor (inhibitory) |
Notes | |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
inhibitor (inhibitory) |
Direct Interaction? | False |
Endogenous Drug? | False |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Mechanism of Interaction | Stem cell growth factor receptor inhibitor |
Direct Interaction | yes |
Specific Action of the Ligand | Inhibition |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
Notes |
inhibitor (inhibitory) |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
Direct Interaction? | False |
inhibitor (inhibitory) |
Details of the Assay for Interaction | Measuring inhibition of kinase activity in a biochemical assay. |
Specific Action of the Ligand | Inhibition |
Endogenous Drug? | False |
KIT | Ensembl Gene Name |
Gene Biotype | PROTEIN_CODING |
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 |
Human Readable Name | DRUGGABLE GENOME |
DRUGGABLE GENOME |
3815 | Entrez Gene ID |
Initial Gene Query | KIT |
Counted Citations from 1950-2000 | 7271 |
KINASE |
MAST/STEM CELL GROWTH FACTOR RECEPTOR KIT | Uniprot Protein Name |
KIT_HUMAN | Uniprot Id |
P10721 | Uniprot Accession |
Interpro Acc | IPR001245 |
Human Readable Name | DRUGGABLE GENOME |
Interpro Type | Domain |
KINASE, DRUGGABLE GENOME |
KIT | Gene Symbol |
Target Class | Receptors |
Target Subclass | EC:2.7.10.1 |
3815 | Entrez Gene Id |
P10721 | Uniprot Accession |
KIT_HUMAN | Uniprot Id |
Target Main Class | Receptors |
Target Subclass | PDGFR |
Target Subclass | KInase |
3815 | Entrez Gene ID |
CancerCommons Reported Gene Name | KIT |
CancerCommons Reported Gene Name | VEGF, PDGF |
CancerCommons Reported Gene Name | Receptor tyrosine kinases KIT, CSF1R, and FLT3 |
6342 | HUGO Gene ID |
6342 | HUGO Gene Symbol |
KIT proto-oncogene, receptor tyrosine kinase | HUGO Gene Name |
GuideToPharmacology Gene Category Name | Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family |
GuideToPharmacology Gene Category ID | 322 |
3815 | CKB Entrez Id |
KIT | CKB Gene Synonym |
C-Kit | CKB Gene Synonym |
PA30128 | PharmGKB ID |
3815 | Entrez Gene ID |
29 | CIViC Gene ID |
DRUG RESISTANCE |
KIT | DrugBank Gene Name |
P10721 | UniProt Accession |
3815 | Entrez Gene Id |
SCFR | GENE_SYMBOL |
KIT | GENE_SYMBOL |
Mast/stem cell growth factor receptor Kit | UNIPROT |
KIT | Gene Symbol |
3815 | Entrez Gene Id |
KIT | MyCancerGenome Gene Symbol |
KIT | MyCancerGenome Reported Gene Name |
ENSG00000157404 | Gene Symbol |
KIT | Ensembl Id |
DRUGGABLE GENOME |
3815 | OncoKB Entrez Id |
PBT | OncoKB Gene Synonym |
C-Kit | OncoKB Gene Synonym |
Mast/stem cell growth factor receptor Kit | Gene Name |
P10721 | UniProt ID |
KINASE, TRANSCRIPTION FACTOR |
SCFR | GO Gene Synonym |
TYROSINE KINASE, EXTERNAL SIDE OF PLASMA MEMBRANE |
KIT | Gene Symbol |
CLINICALLY ACTIONABLE |
3815 | Gene ID |
C-Kit | dGene Synonym |
CD117 | dGene Synonym |
KINASE, TYROSINE KINASE |
KIT | TTD Gene Abbreviation |
T57700 | TTD Target ID |
CLINICALLY ACTIONABLE |
CLINICALLY ACTIONABLE |
CLINICALLY ACTIONABLE |
CLINICALLY ACTIONABLE |
DRUG RESISTANCE |