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Potent VEGFR-2 inhibitor
Potent ATP-competitive VEGFR-2 inhibitor (IC50 = 23 nM). Shows >10-fold selectivity for VEGFR-2 over VEGFR-1. Displays antitumor properties in human lung and colon tumor xenograft models. Orally bioavailable in rodents.
Borzilleri et al (2006) Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2. J.Med.Chem 49 3766 PMID:16789733
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