Description: OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors. Target: Apoptosis, FLT, Raf, c-Fms, Src, CSF-1R, c-Kit, VEGFR. Smiles:...

OSI-930 is a dual inhibitor of Kit (IC50s = 80 and 629 nM for the activated and non-activated kinase, respectively, in cell-free assays) and VEGFR2 (IC50 = 9 nM). It is selective for these kinases over a panel of 17 additional kinases (IC50s = 1.3->10 µM) but also inhibits VEGFR1, CSF1R, C-RAF, and LCK (IC50s = 8,...