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Brivanib alaninate (BMS-582664)

Catalog No. S1138 1 Customer Review(s)

Brivanib alaninate (BMS-582664) Chemical Structure

Bio Information

BMS-582664, also named “brivanib alaninate”, is the alaninate salt of a VEGFR2 inhibitor BMS-540215. Brivanib is hydrolyzed to the active moiety BMS-540215 in vivo. BMS-540215 shows potent and selective inhibition of VEGFR and FGFR tyrosine kinases ^[1,2] . BMS-540215 is an ATP-competitive inhibitor of human VEGFR-2, with an IC50 of 25 nM and Ki of 26 nmol/L. In addition, it inhibits VEGFR-1 (IC50 =380nM) and VEGFR-3 (IC50 = 10 nM). BMS-540215 also showed good selectivity for FGFR-1 (IC50=148 nM), FGFR-2 (IC50 =125 nM), and FGFR-3 (IC50 = 68 nM). Furthermore,BMS-540215 has been shown to selectively inhibit the proliferation of endothelial cells stimulated by VEGF and FGF in vitro with IC50 values of 40 and 276 nM, respectively^[3,4] .
BMS-582664 was prepared in an effort to improve the aqueous solubility and oral bioavailability of the parent compound BMS-540215.

References:

[1] Clin Cancer Res 2008;14:6146-6153

[2] J. Med. Chem 2008;51:1976–1980

[3] Cancer Res 2007;67:6899-6906

[4] Journal of Medicinal Chemistry April 6, 2006;49:2143-2146

Chemical Information

Molecular Weight (WM):	441.46
Formula:	C₂₂H₂₄FN₅O₄

Solubility(R.T.:25°C):	DMSO 88mg/mL
	Water <1mg/mL
	Ethanol 88mg/mL

Quality Control

View current batch:

Purity= 97.71% H-NMR HPLC Purity= 99.32% H-NMR HPLC

Research Area

Protein Tyrosine Kinase >> VEGFR >> VEGFR Inhibitors

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Related Antibodies

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Reactivity: 薛亚红

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Data independently produced by Dr. Yong-Weon Yi from Georgetown University Medical Center
Brivanib alaninate (BMS-582664) purchased from Selleck

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