Annotation Detail

Information
Associated Genes
KIT
Associated Variants
KIT p.Lys643Glu (p.K643E) ( ENST00000288135.6, ENST00000412167.7, ENST00000686011.1, ENST00000687109.1, ENST00000687246.1, ENST00000687295.1, ENST00000689832.1, ENST00000689994.1, ENST00000690543.1, ENST00000692783.1 )
KIT p.Lys643Glu (p.K643E) ( ENST00000288135.6, ENST00000412167.7, ENST00000686011.1, ENST00000687109.1, ENST00000687246.1, ENST00000687295.1, ENST00000689832.1, ENST00000689994.1, ENST00000690543.1, ENST00000692783.1 )
Associated Disease
gastrointestinal stromal tumor
Source Database
CIViC Evidence
Description
The GIST882 patient derived cell line expressing KIT K642E mutation demonstrated sensitivity to ponatinib (IC50: 31nmol/L) and sunitinib (IC50: 54nmol/L) treatments. In comparison, the insensitve KIT-independent GIST226 cell line showed IC50 >2807nmol/L and >5000nmol/L for these drugs respectively. IC50 was determined by assessing cell viability. The GIST882 cell line only showed reduced levels of phospho-KIT and phospho-ERK at high concentrations for ponatinib and sunitinib, while phospho-AKT levels were reduced at all concentrations for ponatinib and sunitinib.
Variant Origin
somatic
Variant Origin
Somatic
Evidence URL
https://civic.genome.wustl.edu/links/evidence_items/7397
Gene URL
https://civic.genome.wustl.edu/links/genes/29
Variant URL
https://civic.genome.wustl.edu/links/variants/978
Rating
3
Evidence Type
Predictive
Disease
Gastrointestinal Stromal Tumor
Evidence Direction
Supports
Drug
Ponatinib,Sunitinib
Evidence Level
D
Clinical Significance
Sensitivity/Response
Pubmed
25239608
Drugs
Drug NameSensitivitySupported
PonatinibSensitivitytrue
SunitinibSensitivitytrue