Brivanib (bms-540215) Inhibitor CAS No. 649735-46-6

Product Name	Brivanib (bms-540215)
Synonyms	Bms-540215
CAS No.	649735-46-6
Molecular Weight	370.38
Formula	C₁₉H₁₉FN₄O₃
Chemical Name	(R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[1,2-f][1,2,4]triazin-6-yloxy)propan-2-ol
Smiles	C(C(C)O)Oc1c(c2n(ncnc2Oc2c(c3cc([nH]c3cc2)C)F)c1)C
Chemical Structure

Biological activities

Brivanib is a dual FGF/VEGF inhibitor. The IC50 of brivanib is 25 nM against human VEGFR-2 while the Ki of brivanib is 26 nM. In addition, brivanib inhibits mouse Flk-1 and FGFR-1 with IC50 of 89 and 148 nM, respectively. In contrast, brivanib also prevents VEGFR-1 with IC50 of 380 nM.^[1] Brivanib induces tumor stasis during the entire 5.5 weeks of therapy.^[2] Brivanib inhibits the new growth of endothelial cells.^[3] Brivanib markedly blocks VEGFR-2, FGFR-1, extracellular signal-regulated kinase 1/2, and Akt phosphorylation in VEGF-stimulated and basic FGF stimulated SK-HEP1 cells.^[4] Brivanib significantly inhibits the growth of H3396 xenografts in athymic mice. At 60 and 90 mg/kg doses, brivanib generates nearly complete inhibition of growth with tumor growth inhibition of 85% and 97%. Brivanib is rapidly absorbed with T_{max of 1 hour, a favorable half-life (t_{1/2) of 2.7 hours, and mean residence time (MRT) of 3.6 hours.^[1]}}

Protocols

In vivo Brivanib is dissolved in PEG400:water (3:2).^[1]

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 active potent VEGFR-2 inhibitor. J Med Chem. 2006. 49(7): 2143-2146. [2] Allen E, et al. Brivanib, a dual FGF/VEGF inhibitor, is active both first and second line against mouse pancreatic neuroendocrine tumors developing adaptive/evasive resistance to VEGF inhibition. Clin Cancer Res. 2011, 17(16): 5299-5310. [3] Ayers M, et al. Discovery and validation of biomarkers that respond to treatment with brivanib alaninate, a small-molecule VEGFR-2/FGFR-1 antagonist. Cancer Res. 2007, 67(14): 6899-6906. [4] Huynh H, et al. Brivanib alaninate, a dual inhibitor of vascular endothelial growth factor receptor and fibroblast growth factor receptor tyrosine kinases, induces growth inhibition in mouse models of human hepatocellular carcinoma. Clin Cancer Res. 2008, 14(19): 6146-6153.

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