Brivanib alaninate（BMS-582664） CAS NO.649735-46-6

brivanib(bms540215) is an atp-competitive inhibitor against vegfr2 with ic50 of 25 nm, moderate potency against vegfr-1 and fgfr-1, but >240-fold against pdgfr-β.
ic50 value: 25 nm
target: vegfr2
in vitro: brivanib also inhibits vegfr1 and fgfr-1 with ic50 of 0.38 μm and 0.148 μm. brivanib is not sensitive to pdgfrβ, egfr, lck, pkcα or jak-3 with ic50 all above 1900 nm. brivanib could inhibit the proliferation of vegf-stimulated huvecs with ic50 of 40 nm, compared to 276 nm in fgf-stimulated huvecs. on the other hand, brivanib exhibits low activity to tumor cell lines [1].
in vivo: brivanib displays antitumor activities in h3396 xenograft in athymic mice. at a dose of 60 and 90 mg/kg (p.o.), brivanib completely inhibits the tumor growth, with tgi of 85% and 97%, respectively [1]. moreover, brivanib significantly suppresses tumor growth in hepatocellular carcinoma (hcc) xenografts, which due to the decrease in phosphorylation of vegfr2. the results show that the tumor weights in 06-0606 xenograft mice are 55% and 13%, compared with the controls at a dose of 50 mg/kg and 100 mg/kg. brivanib is suggested to be efficient in treatment of hcc [2].