Ki8751

Ki8751 is a potent, selective, and orally active small molecule inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2) tyrosine kinase, with an IC50 of 0.9 nM. Originally developed by Kirin Brewery (now Kyowa Kirin), Ki8751 exhibits strong antiangiogenic and antitumor properties. It also displays moderate inhibitory activity against other receptor tyrosine kinases, including c-Kit (IC50 = 40 nM), PDGFRα (IC50 = 67 nM), and FGFR2 (IC50 = 170 nM), while showing high selectivity over other kinases such as EGFR, HGFR, and InsulinR. In preclinical studies, Ki8751 has demonstrated significant inhibition of VEGF-stimulated proliferation of human umbilical vein endothelial cells (HUVECs) and robust antitumor efficacy in various human tumor xenograft models, including glioma, stomach, lung, colon, and melanoma.

Other names

1-(2,4-difluorophenyl)-3-(4-((6,7-dimethoxyquinolin-4-yl)oxy)-2-fluorophenyl)ureaN-(2,4-difluorophenyl)-N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-fluorophenyl]ureaN-(2,4-difluorophenyl)-N'-[4-[(6,7-dimethoxy-4-quinolyl)oxy]-2-fluorophenyl]urea