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Brivanib alaninate (BMS-582664) Chemical Structure
Linifanib (ABT-869)
Linifanib (ABT869) is a structurally novel, potent RTK and VEGF and PDGF receptor families inhibitor for, PDGFR-β, KDR, and CSF-1R, with IC50 of 0.2 nM, 2 nM, 4 nM, and 7 nM, respectively.
Axitinib
Axitinib (AG-013736) is a multiple receptor kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-β and c-KIT with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM, respectively.
BIBF1120 (Vargatef)
BIBF1120 (Vargatef) is a potent VEGF receptor (VEGFR), PDGFR and FGFR kinase inhibitor for VEGFR1, VEGFR2, VEGFR3 with IC50 of 34 nM, 5 nM and 5 nM, respectively.
Cediranib (AZD2171)
Cediranib (AZD2171) is a highly potent VEGFR2 inhibitor for VEGF-stimulated proliferation and KDR phosphorylation with IC50 of 0.4 nM and 0.5 nM, respectively.
Motesanib Diphosphate (AMG-706)
Motesanib (AMG-706) is a multiple inhibitor of VEGFR1/2/3(IC50: 2 ηM /3 ηM /6 ηM),PDGFR (84ηM), kit (8ηM), and Ret (59ηM)receptors
Pazopanib HCl
Pazopanib HCl is a VEGFR inhibitor, IC50 of 10, 30 and 47 nM for VEGFR-1, -2, and -3.
Sorafenib (Nexavar)
Sorafenib (Nexavar) is a novel, small molecular inhibitor of several tyrosine protein kinases (VEGFR and PDGFR) and RAF/MEK/ERK cascade inhibitor with an IC50 of 6, 22, 38 nM for Raf-1, wt BRAF and V599E mutant BRAF.
Sunitinib Malate (Sutent)
Sunitinib (Sutent) is a multitargeted FLT3, PDGFRs, VEGFRs, and Kit kinase inhibitor with Ki of 0.009 and 0.008 μM for Flk-1 and PDGFR
Vandetanib (Zactima)
Vandetanib (Zactima) is a VEGFR and EGFR antagonist and a tyrosine kinase inhibitor with IC50 of 60, 90, 40 nM for HUVEC proliferation, PC-9 cells and tyrosine kinase activity, respectively.
Masitinib
Masitinib also known as Masivet, AB1010 is a tyrosine kinase, c-Kit, PDGFR, FGFR3, the FAK pathway inhibitor with IC50 of 150 ± 80, 200 ± 40 n
Biological Activity
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 on Brivanib alaninate (BMS-582664)
- [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
Product Information
| Molecular Weight (WM): | 441.46 |
|---|---|
| Formula: | C22H24FN5O4 |
| CAS No.: | 649735-63-7 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥88mg/mL |
| Water <1mg/mL | |
| Ethanol ≥88mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
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