Vatalanib is a potent, selective, orally active inhibitor of the VEGFR tyrosine kinases VEGFR-1 (Flt-1, IC50 = 77 nM) and VEGFR-2 (FLK-1/KDR, IC50 = 37 nM), with slightly higher potency against the latter. At higher concentrations, other tyrosine kinases are also inhibited, including PDGFR-ß (IC50 = 580 nM), c-KIT (IC50 = 730 nM), FLT-4 (IC50 = 660 nM) and c-FMS (IC50 = 1.4 µM). On the other hand, vatalanib is not active against the EGFR, c-SRC, v-ABL, and protein kinase Cα (IC50 > 10 µM)
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