v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog

Target id: 1805

Nomenclature: v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog

Abbreviated Name: Kit

Family: Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family

Annotation status:  image of an orange circle Annotated and awaiting review. Please contact us if you can help with reviewing.  » Email us

Gene and Protein Information
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 976 4q11-q12 KIT v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog
Mouse 1 979 5 Kit kit oncogene
Rat - 978 14p11 Kit v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog
Previous and Unofficial Names
CD117
C-Kit
PBT
stem cell growth factor receptor
piebald trait
c-kit receptor tyrosine kinase
mast/stem cell growth factor receptor
p145 c-kit
Proto-oncogene c-Kit
Steel Factor Receptor
Database Links
BRENDA
Ensembl Gene
Entrez Gene
ExplorEnz
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Enzyme
KEGG Gene
NeXtProt
OMIM
Orphanet
PhosphoSitePlus
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene
UniProtKB
Wikipedia
Selected 3D Structures
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the extracellular domain of the receptor tyrosine kinase, Kit
PDB Id:  2EC8
Resolution:  3.0Å
Species:  Human
References:  31
Image of receptor 3D structure from RCSB PDB
Description:  KIT kinase domain in complex with sunitinib
PDB Id:  3G0E
Ligand:  sunitinib
Resolution:  1.6Å
Species:  Human
References:  11
Enzyme Reaction
EC Number: 2.7.10.1
Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
sunitinib Hs Inhibition 9.43 pKd 7
pKd 9.43 (Kd 3.7x10-10 M) [7]
AC710 Hs Inhibition 9.0 pKd 19
pKd 9.0 (Kd 1x10-9 M) [19]
quizartinib Hs Inhibition 8.32 pKd 5
pKd 8.32 (Kd 4.8x10-9 M) [5]
masitinib Hs Inhibition 8.09 pKd 7
pKd 8.09 (Kd 8.1x10-9 M) [7]
crenolanib Hs Inhibition 7.11 pKd 15
pKd 7.11 (Kd 7.8x10-8 M) [15]
famitinib Hs Inhibition 8.7 pIC50 6
pIC50 8.7 (IC50 2x10-9 M) [6]
dovitinib Hs Inhibition 8.52 – 8.7 pIC50 24,27
pIC50 8.52 – 8.7 (IC50 3x10-9 – 2x10-9 M) [24,27]
cediranib Hs Inhibition 8.52 pIC50 28
pIC50 8.52 (IC50 3x10-9 M) [28]
compound 7k [PMID 23521020] Hs Inhibition 8.31 pIC50 12
pIC50 8.31 (IC50 4.89x10-9 M) [12]
JNJ-28312141 Hs Inhibition 8.3 pIC50 20
pIC50 8.3 (IC50 5x10-9 M) [20]
SU11652 Hs Inhibition 8.0 pIC50 10
pIC50 8.0 (IC50 1x10-8 M) [10]
compound 8h [PMID 22765894] Hs Inhibition 7.96 pIC50 18
pIC50 7.96 (IC50 1.1x10-8 M) [18]
sunitinib Hs Inhibition 7.88 pIC50 17
pIC50 7.88 (IC50 1.31x10-8 M) [17]
linifanib Hs Inhibition 7.85 pIC50 2
pIC50 7.85 (IC50 1.4x10-8 M) [2]
SU-14813 Hs Inhibition 7.82 pIC50 23
pIC50 7.82 (IC50 1.5x10-8 M) [23]
AKN-028 Hs Inhibition 7.54 pIC50 9
pIC50 7.54 (IC50 2.9x10-8 M) [9]
Description: Inhibition of KIT autophosphorylation in human AML M07 cells which overexpress KIT
sorafenib Hs Inhibition 7.17 pIC50 29
pIC50 7.17 (IC50 6.8x10-8 M) [29]
pazopanib Hs Inhibition 6.85 pIC50 14
pIC50 6.85 (IC50 1.4x10-7 M) [14]
tandutinib Hs Inhibition 6.77 pIC50 16
pIC50 6.77 (IC50 1.7x10-7 M) [16]
masitinib Hs Inhibition 6.7 pIC50 8
pIC50 6.7 (IC50 2x10-7 M) [8]
CP-673451 Hs Inhibition 6.6 pIC50 25
pIC50 6.6 (IC50 2.52x10-7 M) [25]
GTP-14564 Hs Inhibition 6.52 pIC50 21
pIC50 6.52 (IC50 3x10-7 M) [21]
semaxanib Hs Inhibition 6.4 pIC50 4
pIC50 6.4 (IC50 4x10-7 M) [4]
apatinib Hs Inhibition 6.37 pIC50 26
pIC50 6.37 (IC50 4.29x10-7 M) [26]
Description: Assay used apatinib mesylate (YN968D1)
Ki-20227 Hs Inhibition 6.35 pIC50 22
pIC50 6.35 (IC50 4.51x10-7 M) [22]
AST-487 Hs Inhibition 6.3 pIC50 1
pIC50 6.3 (IC50 5x10-7 M) [1]
Description: In vitro inhibition of c-Kit
lucitanib Hs Inhibition 6.28 pIC50 32
pIC50 6.28 (IC50 5.27x10-7 M) [32]
DiscoveRx KINOMEscan® screen
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 7,30

Key to terms and symbols Click column headers to sort
Target used in screen: KIT
Ligand Sp. Type Action Affinity Units
sunitinib Hs Inhibitor Inhibition 9.43 pKd
cediranib Hs Inhibitor Inhibition 9.42 pKd
SU-14813 Hs Inhibitor Inhibition 9.17 pKd
Ki-20227 Hs Inhibitor Inhibition 9.16 pKd
dasatinib Hs Inhibitor Inhibition 9.09 pKd
PD-173955 Hs Inhibitor Inhibition 8.74 pKd
linifanib Hs Inhibitor Inhibition 8.7 pKd
foretinib Hs Inhibitor Inhibition 8.6 pKd
tandutinib Hs Inhibitor Inhibition 8.57 pKd
pazopanib Hs Inhibitor Inhibition 8.55 pKd
Target used in screen: KIT(A829P)
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 9.22 pKd
dasatinib Hs Inhibitor Inhibition 9.18 pKd
foretinib Hs Inhibitor Inhibition 8.49 pKd
tamatinib Hs Inhibitor Inhibition 8.46 pKd
quizartinib Hs Inhibitor Inhibition 8.44 pKd
AST-487 Hs Inhibitor Inhibition 8.36 pKd
masitinib Hs Inhibitor Inhibition 7.92 pKd
motesanib Hs Inhibitor Inhibition 7.82 pKd
imatinib Hs Inhibitor Inhibition 7.82 pKd
linifanib Hs Inhibitor Inhibition 7.77 pKd
Target used in screen: KIT(D816H)
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 9.37 pKd
dasatinib Hs Inhibitor Inhibition 8.8 pKd
tamatinib Hs Inhibitor Inhibition 8.19 pKd
lestaurtinib Hs Inhibitor Inhibition 7.96 pKd
midostaurin Hs Inhibitor Inhibition 7.8 pKd
foretinib Hs Inhibitor Inhibition 7.44 pKd
JNJ-28312141 Hs Inhibitor Inhibition 7.32 pKd
AST-487 Hs Inhibitor Inhibition 7.17 pKd
sunitinib Hs Inhibitor Inhibition 6.96 pKd
tandutinib Hs Inhibitor Inhibition 6.92 pKd
Target used in screen: KIT(D816V)
Ligand Sp. Type Action Affinity Units
staurosporine Hs Inhibitor Inhibition 9.19 pKd
tamatinib Hs Inhibitor Inhibition 8.6 pKd
dasatinib Hs Inhibitor Inhibition 8.59 pKd
lestaurtinib Hs Inhibitor Inhibition 8.15 pKd
midostaurin Hs Inhibitor Inhibition 8.11 pKd
foretinib Hs Inhibitor Inhibition 8.02 pKd
JNJ-28312141 Hs Inhibitor Inhibition 7.74 pKd
NVP-TAE684 Hs Inhibitor Inhibition 7.59 pKd
tandutinib Hs Inhibitor Inhibition 7.54 pKd
PD-173955 Hs Inhibitor Inhibition 7.46 pKd
Target used in screen: KIT(L576P)
Ligand Sp. Type Action Affinity Units
SU-14813 Hs Inhibitor Inhibition 9.54 pKd
cediranib Hs Inhibitor Inhibition 9.27 pKd
dasatinib Hs Inhibitor Inhibition 9.24 pKd
Ki-20227 Hs Inhibitor Inhibition 9.07 pKd
motesanib Hs Inhibitor Inhibition 8.89 pKd
sunitinib Hs Inhibitor Inhibition 8.89 pKd
dovitinib Hs Inhibitor Inhibition 8.8 pKd
axitinib Hs Inhibitor Inhibition 8.77 pKd
pazopanib Hs Inhibitor Inhibition 8.74 pKd
linifanib Hs Inhibitor Inhibition 8.72 pKd
Target used in screen: KIT(V559D)
Ligand Sp. Type Action Affinity Units
cediranib Hs Inhibitor Inhibition 9.57 pKd
sunitinib Hs Inhibitor Inhibition 9.39 pKd
Ki-20227 Hs Inhibitor Inhibition 9.34 pKd
axitinib Hs Inhibitor Inhibition 9.31 pKd
SU-14813 Hs Inhibitor Inhibition 9.29 pKd
dasatinib Hs Inhibitor Inhibition 9.17 pKd
PD-173955 Hs Inhibitor Inhibition 8.8 pKd
linifanib Hs Inhibitor Inhibition 8.77 pKd
foretinib Hs Inhibitor Inhibition 8.68 pKd
pazopanib Hs Inhibitor Inhibition 8.64 pKd
Target used in screen: KIT(V559D,T670I)
Ligand Sp. Type Action Affinity Units
sunitinib Hs Inhibitor Inhibition 9.55 pKd
cediranib Hs Inhibitor Inhibition 9.49 pKd
SU-14813 Hs Inhibitor Inhibition 9.25 pKd
axitinib Hs Inhibitor Inhibition 8.85 pKd
foretinib Hs Inhibitor Inhibition 8.62 pKd
linifanib Hs Inhibitor Inhibition 8.42 pKd
quizartinib Hs Inhibitor Inhibition 8.22 pKd
pazopanib Hs Inhibitor Inhibition 8.19 pKd
barasertib-hQPA Hs Inhibitor Inhibition 8.1 pKd
staurosporine Hs Inhibitor Inhibition 8.02 pKd
Target used in screen: KIT(V559D,V654A)
Ligand Sp. Type Action Affinity Units
sunitinib Hs Inhibitor Inhibition 9.68 pKd
SU-14813 Hs Inhibitor Inhibition 9.6 pKd
cediranib Hs Inhibitor Inhibition 9.51 pKd
dasatinib Hs Inhibitor Inhibition 8.57 pKd
dovitinib Hs Inhibitor Inhibition 8.51 pKd
Ki-20227 Hs Inhibitor Inhibition 8.49 pKd
axitinib Hs Inhibitor Inhibition 8.46 pKd
masitinib Hs Inhibitor Inhibition 8.33 pKd
JNJ-28312141 Hs Inhibitor Inhibition 8.22 pKd
foretinib Hs Inhibitor Inhibition 8.12 pKd
Target used in screen: KIT-autoinhibited
Ligand Sp. Type Action Affinity Units
dasatinib Hs Inhibitor Inhibition 8.92 pKd
sunitinib Hs Inhibitor Inhibition 8.52 pKd
Ki-20227 Hs Inhibitor Inhibition 7.27 pKd
PD-173955 Hs Inhibitor Inhibition 7.04 pKd
quizartinib Hs Inhibitor Inhibition 6.72 pKd
staurosporine Hs Inhibitor Inhibition 6.34 pKd
AST-487 Hs Inhibitor Inhibition 5.92 pKd
vatalanib Hs Inhibitor Inhibition 5.82 pKd
sorafenib Hs Inhibitor Inhibition 5.66 pKd
imatinib Hs Inhibitor Inhibition 5.35 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx


Reference: 3,13

Key to terms and symbols Click column headers to sort
Target used in screen: cKit/c-Kit
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
dasatinib Hs Inhibitor Inhibition 3.3
sunitinib Hs Inhibitor Inhibition 8.7
staurosporine Hs Inhibitor Inhibition 8.7 9.5 1.0
dovitinib Hs Inhibitor Inhibition 9.9
pazopanib Hs Inhibitor Inhibition 10.9
Flt-3 inhibitor III Hs Inhibitor Inhibition 20.3 1.0 1.0
dorsomorphin Hs Inhibitor Inhibition 21.4 5.0 2.0
Lck inhibitor Hs Inhibitor Inhibition 21.6 36.0 1.0
PDK1/Akt/Flt dual pathway inhibitor Hs Inhibitor Inhibition 22.2 114.0 96.0
PDGF receptor tyrosine kinase inhibitor IV Hs Inhibitor Inhibition 27.9 0.0 0.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Clinically-Relevant Mutations and Pathophysiology
Disease:  Acute myeloblastic leukemia with maturation
Orphanet: ORPHA98834
Disease:  Acute myeloid leukemia
Synonyms: Acute myelogenous leukemia
Disease Ontology: DOID:9119
OMIM: 601626
Orphanet: ORPHA519
Disease:  Acute myeloid leukemia with abnormal bone marrow eosinophils
Orphanet: ORPHA98829
Disease:  Acute myeloid leukemia with t(8;21)(q22;q22) translocation
Orphanet: ORPHA102724
Disease:  Aleukemic mast cell leukemia
Orphanet: ORPHA158799
Disease:  Bullous diffuse cutaneous mastocytosis
Orphanet: ORPHA280785
Disease:  Classic mast cell leukemia
Orphanet: ORPHA158796
Disease:  Cutaneous mastocytoma
Orphanet: ORPHA79455
Disease:  Gastrointestinal stromal tumor
Disease Ontology: DOID:9253
OMIM: 606764
Orphanet: ORPHA44890
Comments: 
Disease:  Isolated bone marrow mastocytosis
Orphanet: ORPHA158778
Disease:  Lymphoadenopathic mastocytosis with eosinophilia
Orphanet: ORPHA158793
Disease:  Mast cell disease
Synonyms: Maculopapular cutaneous mastocytosis [Orphanet: ORPHA79457]
Typical urticaria pigmentosa [Orphanet: ORPHA158766]
Urticaria pigmentosa [Disease Ontology: DOID:12309]
Disease Ontology: DOID:12309
OMIM: 154800
Orphanet: ORPHA79457, ORPHA158766
Disease:  Nodular urticaria pigmentosa
Orphanet: ORPHA158772
Disease:  Piebaldism
Synonyms: Piebald trait [OMIM: 172800]
Disease Ontology: DOID:3263
OMIM: 172800
Orphanet: ORPHA2884
Disease:  Plaque-form urticaria pigmentosa
Orphanet: ORPHA158769
Disease:  Pseudoxanthomatous diffuse cutaneous mastocytosis
Orphanet: ORPHA280794
Disease:  Smouldering systemic mastocytosis
Orphanet: ORPHA158775
Disease:  Systemic mastocytosis with an associated clonal hematologic non-mast cell lineage disease
Orphanet: ORPHA98849
Disease:  Telangiectasia macularis eruptiva perstans
Orphanet: ORPHA90389
Disease:  Testicular germ cell tumor
Synonyms: Seminoma [Disease Ontology: DOID:4440]
Testicular pure germ cell tumor [Disease Ontology: DOID:4087]
Disease Ontology: DOID:4087, DOID:4440
OMIM: 273300

References

Show »

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How to cite this page

Type III RTKs: PDGFR, CSFR, Kit, FLT3 receptor family: v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog. Last modified on 11/03/2015. Accessed on 25/05/2015. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=1805.