Ki8751 is a potent, selective and orally active VEGFR-2 inhibitor that inhibits VEGFR-2 phosphorylation with IC50 of 0.6 nM.
Ki8751 also inhibits PDGFR family members such as PDGFRα and c-Kit at 67 nM and 40 nM, does not have any inhibitory activity against other kinases such as EGFR, HGFR, InsulinR (IC50>10 uM).
Ki8751 suppressed the growth of the VEGF-stimulated HUVEC on nanomolar level, shows significant antitumor activity against human tumor xenografts such as glioma, stomach carcinoma), lung carcinoma, colon carcinoma and melanoma in nude mice.
