YM-359445

A highly potent, orally active VEGFR-2 inhibitor with IC50 of 8.5 nM, without activity against PKA, PKCα, PDK-1 and JNK3 (IC50>1 uM); inhibits VEGFR2 tyrosine kinase activity completely at 0.03 uM, inhibits HUVEC proliferation induced by VEGF with IC50 of 1.5 nM; inhibits VEGF-stimulated autophosphorylation of VEGFR2 at 0.1 nM, also inhibits sprout formation of endothelial cells at 3 nM; not only inhibits tumor growth but also reduces its vasculature in mice bearing various tumors, including paclitaxel-resistant tumors.

References 1. Amino N, et al. Clin Cancer Res. 2006 Mar 1;12(5):1630-8. View Related Products by Target VEGFR