AMG 706 is a multikinase inhibitor that predominantly targets receptor tyrosine kinases, including VEGFR1, VEGFR2, VEGFR3, c-Kit, PDGFR, and RET (IC50s = 2, 3, 6, 8, 84, and 59 nM, respectively). It also potently inhibits CSF1R and ZAK (IC50s = 5.6 and 8 nM, respectively), as well as several mutants of c-Kit. AMG 706 inhibits the proliferation of human endothelial cells induced by VEGF but not FGF. Oral administration of AMG 706 blocks VEGF-induced angiogenesis in the rat corneal model and induces regression of established A431 xenografts in mice.
