Brivanib alaninate
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Brivanib alaninate
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CAS No:
649735-63-7
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Formula:
C22H24FN5O4
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Chemical Name:
Brivanib alaninate
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Synonyms:
L-Alanine,(1R)-2-[[4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxy]-1-methylethyl ester;BMS 582664;Brivanib alaninate;924262-84-0
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CAS No:
Description
Brivanib alaninate is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ.
Brivanib alaninate is a carboxylic ester resulting from the formal condensation of the carboxy group of L-alanine with the hydroxy group of brivanib. It is a prodrug of brivanib (BMS-540215), a potent oral dual inhibitor of VEGFR-2 and FGFR-1 (IC50 of 25 nM and 148 nM, respectively) and was in development for the treatment of hepatocellular and colon carcinomas. It has a role as an antineoplastic agent, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, a prodrug, an apoptosis inducer, a fibroblast growth factor receptor antagonist and an angiogenesis inhibitor. It is a pyrrolotriazine, an aromatic ether, a fluoroindole, a diether, a carboxylic ester and a L-alanine derivative. It derives from a brivanib.|Brivanib alaninate has been investigated for the treatment of Colorectal Cancer.|Brivanib Alaninate is the alaninate salt 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.
Safety Information
Ⅲ
2811
6.1
P201, P202, P260, P264, P270, P281, P301+P312, P308+P313, P314, P330, P405, P501
H302
Brivanib alaninate Use and Manufacturing
BMS-582664 is an oral VEGFR/FGFR inhibitor for VEGFR2, Flk1, VEGFR1 and FGFR1 with IC50 of 25 nM, 89 nM, 380 nM and 148 nM, respectively.
Human drugs -> Rare disease (orphan)
Computed Properties
Molecular Weight:441.5
XLogP3:3.1
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:8
Rotatable Bond Count:8
Exact Mass:441.18123243
Monoisotopic Mass:441.18123243
Topological Polar Surface Area:117
Heavy Atom Count:32
Complexity:660
Defined Atom Stereocenter Count:2
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes
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