Brivanib (CAS 649735-46-6)

Brivanib is an inhibitor of the vascular endothelial growth factor receptor (VEGFR). Through inhibition of the Brivanib family of receptors involved in angiogenesis, Brivanib effectively blocks the formation of new blood vessels. In addition to its angiogenesis-inhibiting properties, Brivanib has exhibited multiple biological activities. Numerous studies have demonstrated its ability to inhibit the growth of diverse cancer cell lines. Moreover, Brivanib has displayed anti-inflammatory effects in cultured macrophages and has shown promise in improving cardiac function in heart failure models. Brivanib functions as an ATP-competitive inhibitor, specifically targeting human Flk-1 (VEGFR-2) and mouse Flk-1 with IC50 values of 25 nM and 89 nM, respectively. It also inhibits Flt-1 (VEGFR-1) and Flg (FGFR-1) with IC50 values of 0.38 μM and 0.148 μM, respectively. Notably, Brivanib exhibits significant antitumor activities in H3396 xenograft models, completely inhibiting tumor growth with TGI values of 85% and 97%.