Ki8751

Ki8751 is a potent, selective inhibitor of VEGFR-2 tyrosine kinase (IC50 = 0.9 nM). Ki8751 suppressed the growth of the VEGF-stimulated human umbilical vein endothelial cell (HUVEC) and inhibits tumor growth in vivo. Ki8751 also inhibited the PDGFR family members such as PDGFRalpha and c-Kit at 67 nM and 40 nM, respectively. Ki8751 (10 nM) increases cellular senescence in metastatic colorectal cancer (CRC) cells MIP, RKO, SW620 and SW480. Ki8751 showed significant antitumor activity against five human tumor xenografts such as GL07 (glioma), St-4 (stomach carcinoma), LC6 (lung carcinoma), DLD-1 (colon carcinoma) and A375 (melanoma) in nude mice. Ki8751 also showed complete tumor growth inhibition with the LC-6 xenograft in nude rats following oral administration once a day for 14 days at 5 mg/kg without any body weight loss.