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Biological Activity:
Motesanib (AMG 706) is a novel oral inhibitor of VEGF receptors, platelet-derived growth-factor receptor,and KIT. AMG 706 potently inhibited VEGF-induced but not bFG-induced proliferation of HUVECs with IC50 values of 10 nmol/L and>3000 nmol/L, respectively. Similarly,AMG 706 potently inhibited both PDGFinduced proliferation and SCFinduced c-kit phosphorylation with IC50 values of 207 and 37 nmol/L, respectively.
References:
Polverino A, et al. AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer Res, 2006, 66(17), 8715-8721.