WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 200570
CAS#: 649735-63-7 (alaninate)
Description: Brivanib alaninate is the alaninate ester 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.
MedKoo Cat#: 200570
Name: Brivanib alaninate
CAS#: 649735-63-7 (alaninate)
Chemical Formula: C22H24FN5O4
Exact Mass: 441.18123
Molecular Weight: 441.45
Elemental Analysis: C, 59.86; H, 5.48; F, 4.30; N, 15.86; O, 14.50
Brivanib alaninate (BMS-582664),purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.
Synonym: BMS582664; BMS-582664; BMS 582664; Brivanib alaninate
IUPAC/Chemical Name: (S)-(R)-1-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)oxy)propan-2-yl 2-aminopropanoate
InChi Key: LTEJRLHKIYCEOX-GXTWGEPZSA-N
InChi Code: InChI=1S/C22H24FN5O4/c1-11-7-15-16(27-11)5-6-17(19(15)23)32-21-20-13(3)18(8-28(20)26-10-25-21)30-9-12(2)31-22(29)14(4)24/h5-8,10,12,14,27H,9,24H2,1-4H3/t12-,14+/m0/s1
SMILES Code: C[C@@H](N)C(O[C@@H](C)COC1=CN2N=CN=C(OC3=C(F)C4=C(NC(C)=C4)C=C3)C2=C1C)=O
The following data is based on the product molecular weight 441.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Finn RS, Kang YK, Mulcahy M, Polite BN, Lim HY, Walters I, Baudelet C, Manekas D, Park JW. Phase II, Open-label Study of Brivanib as Second-line Therapy in Patients with Advanced Hepatocellular Carcinoma. Clin Cancer Res. 2012 Jan 11. [Epub ahead of print] PubMed PMID: 22238246.
2: Gong J, Gan J, Iyer RA. Identification of the oxidative and conjugative enzymes involved in the biotransformation of brivanib. Drug Metab Dispos. 2012 Jan;40(1):219-26. Epub 2011 Oct 11. PubMed PMID: 21989950.
3: Garcia JA, Roberts LR. Phase II, open-label study of brivanib as first-line therapy in patients with advanced hepatocellular carcinoma. J Hepatol. 2011 Sep 29. [Epub ahead of print] PubMed PMID: 21963517.
4: Kudo M. Future treatment option for hepatocellular carcinoma: a focus on brivanib. Dig Dis. 2011;29(3):316-20. Epub 2011 Aug 9. Review. PubMed PMID: 21829023.
5: Syed S, Clemens PL, Lathers D, Kollia G, Dhar A, Walters I, Masson E. Lack of Effect of Brivanib on the Pharmacokinetics of Midazolam, a CYP3A4 Substrate, Administered Intravenously and Orally in Healthy Participants. J Clin Pharmacol. 2011 Jun 9. [Epub ahead of print] PubMed PMID: 21659627.
6: Garrett CR, Siu LL, El-Khoueiry A, Buter J, Rocha-Lima CM, Marshall J, LoRusso P, Major P, Chemidlin J, Mokliatchouk O, Velasquez L, Hayes W, Feltquate D, Syed S, Ford S, Kollia G, Galbraith S, Nuyten DS. Phase I dose-escalation study to determine the safety, pharmacokinetics and pharmacodynamics of brivanib alaninate in combination with full-dose cetuximab in patients with advanced gastrointestinal malignancies who have failed prior therapy. Br J Cancer. 2011 Jun 28;105(1):44-52. doi: 10.1038/bjc.2011.182. Epub 2011 May 31. PubMed PMID: 21629245; PubMed Central PMCID: PMC3137402.
7: Allen E, Walters IB, Hanahan D. 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 Aug 15;17(16):5299-310. doi: 10.1158/1078-0432.CCR-10-2847. Epub 2011 May 27. PubMed PMID: 21622725; PubMed Central PMCID: PMC3156934.
8: LoRusso P, Shapiro GI, Hurwitz H, Pilat MJ, Chemidlin J, Kollia G, Syed S, Fischer B, Masson E. Lack of food effect on single-dose pharmacokinetics of brivanib, and safety and efficacy following multiple doses in subjects with advanced or metastatic solid tumors. Cancer Chemother Pharmacol. 2011 Dec;68(6):1377-85. Epub 2011 Apr 3. PubMed PMID: 21461891.
9: Diaz-Padilla I, Siu LL. Brivanib alaninate for cancer. Expert Opin Investig Drugs. 2011 Apr;20(4):577-86. Epub 2011 Mar 11. Review. PubMed PMID: 21391890.
10: Park JW, Finn RS, Kim JS, Karwal M, Li RK, Ismail F, Thomas M, Harris R, Baudelet C, Walters I, Raoul JL. Phase II, open-label study of brivanib as first-line therapy in patients with advanced hepatocellular carcinoma. Clin Cancer Res. 2011 Apr 1;17(7):1973-83. Epub 2011 Feb 24. PubMed PMID: 21349999.