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BMS 540215
- Brivanib
- Optical Purity: Optically pure
- Soluble in DMSO
- MF: C19H19FN4O3
- MW: 370.38
Description
BMS 540215 (Brivanib) is an ATP-competitive VEGFR and FGFR receptor tyrosine kinase inhibitor with reported IC50 values of 25 nM, 380 nM and 10 nM for VEGFR2, VEGFR1 and VEGFR3, respectively.
VEGF and FGF receptor signaling regulate angiogenesis, endothelial cell proliferation and tumor vascularization. BMS 540215 is useful for studying dual angiogenic pathway inhibition. BMS 540215 is the active component of its prodrug, Brivalib alaninate (also known as BMS 582664, Axon 1864), which hydrolyzes to BMS 540215 in vivo rapidly.
Key Features
- ATP-competitive VEGFR/FGFR inhibitor
- IC50: 25 nM for VEGFR2, 380 nM for VEGFR1 and 10 nM for VEGFR3
- Also inhibits FGFR1, FGFR2 and FGFR3 in the nanomolar range
- Targets angiogenesis-associated receptor tyrosine kinase signaling
Applications
- VEGF and FGF pathway research
- Angiogenesis and endothelial cell assays
- Tumor vascularization models
- RTK inhibitor selectivity and pathway profiling
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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