KIT(V559D,V654A)
KINASE INFORMATION
Kinase Name
v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog
Entrez Gene Symbol
KIT
Entrez Gene ID
3815
Aliases
CD117; C-Kit; KIT; PBT; SCFR
Kinase Group
TK
Species
Human
PROTEIN INFORMATION
Accession #
NP_000213.1
Kinase Construct
Partial Length
Kinase Form
Mutation (V559D,V654A)
Mutation Relevance
V654A mutation confers imatinib-resistance in gastrointestinal stromal tumors (GIST).
Mutation References
Clin Cancer Res.
11, 4182-4190 (2005)
Expression System
Bacterial
ASSAY INFORMATION
Average Z’ Value
0.71
Panel
scanELECT; scanMAX; scanTK;
REFERENCE INHIBITOR INFORMATION
Compound
Kd
AMG-706
23 nM
AST-487
100 nM
Imatinib
71 nM
MLN-518
26 nM
PKC-412
1600 nM
Sunitinib
0.21 nM