Cat No.
CEI-0011
Description
Sunitinib Malate (Sutent) can inhibit VEGFR2 (Flk-1) and PDGFRbeta with IC50 of 80 nM and 2 nM.
Alias
SU-11248
Synonyms
SU-11248
CAS No.
341031-54-7
Targets
VEGFR2, PDGFRbeta
Chemical Name
(Z)-N-(2-(diethylamino)ethyl)-5-((5-fluoro-2-oxoindolin-3-ylidene)methyl)-2,4-dimethyl-1H-pyrrole-3-carboxamide,(S)-2-hydroxysuccinic acid
M.Wt
532.56
Purity
>99%
Solubility
DSMO 5 mg/mL Water
Storage
2 years at -20 centigrade
In vitro
By competing with ATP for binding within the intracellular domain of various wild-type and/or mutated receptor tyrosine kinases, sunitinib (SU11248) inhibit a list of tyrosine kinase including endothelial growth factor receptors (VEGFR-1, VEGFR-2, and VEGFR-3), platelet-derived growth factor receptors (PDGFR-alpha and PDGFR- beta ), fms-related tyrosine kinase 3 (FLT3), stem cell growth factor receptor KIT, and RET. As a multitargeted agent, sunitinib achieves a broader spectrum of activity than single-target agents including erlotinib and gefitinib. Sunitinib shows great inhibition to many cancer cells including gastrointestinal stromal tumours (GIST) and renal-cell carcinoma (RCC).
