Brivanib alaninate
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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.


Price and Availability

Size Price Shipping out time Quantity
5mg USD 270 2 Weeks
10mg USD 455 2 Weeks
25mg USD 835 2 Weeks
50mg USD 1600 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-06-06. Prices are subject to change without notice.

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.


Chemical Structure

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Theoretical Analysis

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


Related CAS #: 649735-46-6   649735-63-7 (alaninate)    

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


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

 
 


References

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.