Product Data SheetProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :Brivanib9735-46-6HY-10337370.38C19H19FN4O3>98%ySolubility:gDMSO ≥70mg/mL Water<1.2mg/mL Ethanol ≥4.8mg/mLMechanisms: Pathways:Protein Tyrosine Kinase/RTK; Target:VEGFR Biological Activity:Brivanib(BMS540215) is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM,Brivanib(BMS540215)isanATPcompetitiveinhibitoragainstVEGFR2withIC50of25nMmoderate 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 isnot sensitive to PDGFRβ, EGFR, LCK, PKCα or JAK-3 with IC50 all above 1900 nM. Brivanib couldinhibit the proliferation of VEGF-stimulated HUVECs with IC50 of 40 nM, compared to 276 nM inFGF-stimulated HUVECs. On the other hand, Brivanib exhibits low activity to tumor cell lines [1]. pygyin vivo: Brivanib displays antitumor activities in H3396 xenograft in athymic mice. At a dose of 60and 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 Hepatocellularcarcinoma (HC...References:[1]. Bhide RS, et al. Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo activepotent VEGFR-2 inhibitor. J Med Chem, 2006, 49 (7), 2143-2146. [2]. Huynh H, et al. Brivanib alaninate, a dual inhibitor of vascular endothelial growth factor receptorand fibroblast growth factor receptor tyrosine kinases, induces growth inhibition in mouse models ofhuman hepatocellular carcinoma. Clin Cancer Res, 2008, 14(19), 6146-6153. Caution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 08540,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr
