Brivanib Alaninate RC02564

Brivanib alaninate is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ.
Brivanib alaninate is a carboxylic ester resulting from the formal condensation of the carboxy group of L-alanine with the hydroxy group of brivanib. It is a prodrug of brivanib (BMS-540215), a potent oral dual inhibitor of VEGFR-2 and FGFR-1 (IC50 of 25 nM and 148 nM, respectively) and was in development for the treatment of hepatocellular and colon carcinomas. It has a role as an antineoplastic agent, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, a prodrug, an apoptosis inducer, a fibroblast growth factor receptor antagonist and an angiogenesis inhibitor. It is a pyrrolotriazine, an aromatic ether, a fluoroindole, a diether, a carboxylic ester and a L-alanine derivative. It derives from a brivanib.|Brivanib alaninate has been investigated for the treatment of Colorectal Cancer.|Brivanib Alaninate is the alaninate salt of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib strongly binds to and inhibits VEGFR2, a tyrosine kinase receptor expressed almost exclusively on vascular endothelial cells; inhibition of VEGFR2 may result in inhibition of tumor angiogenesis, inhibition of tumor cell growth, and tumor regression.