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BMS 540215
- Brivanib
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C19H19FN4O3
- MW: 370.38
Description
Potent and ATP-competitive inhibitor of VEGF; it inhibits VEGFR2, -1 and -3 with IC50 of 25, 380 and 10 nM respectively; also showed good selectivity for FGFR-1, -2, and -3 with IC50 of 148, 125 and 68 nM. BMS 540215 is the active component of its prodrug, Brivalib alaninate (BMS 582664, Axon 1864), which hydrolyzes to BMS 540215 in vivo quickly
More Information
| Parent CAS No. | 649735-46-6 |
|---|---|
| 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(OC1=CN2C(=C1C)C(OC1C=CC3=C(C=1F)C=C(C)N3)=NC=N2)[C@H](O)C |&1:24,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C19H19FN4O3/c1-10-6-13-14(23-10)4-5-15(17(13)20)27-19-18-12(3)16(26-8-11(2)25)7-24(18)22-9-21-19/h4-7,9,11,23,25H,8H2,1-3H3/t11-/m1/s1 |
| InChiKey | WCWUXEGQKLTGDX-LLVKDONJSA-N |
| CID | 11234052 |
| Short Description | VEGFR inhibitor |
References
- RS Bhide 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.
- ZW Cai et al. Discovery of brivanib alaninate ((S)-((R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), a novel prodrug of dual vascular (...). J. Med. Chem. 2008, 51(6), 1976-1980.
- H Huynh 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 (...). Clin. Cancer Res. 2008, 14, 6146.
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