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Brivanib

Catalog No. T6036 CAS 649735-46-6

Synonyms: BMS-540215

Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but <240-fold against PDGFR-β. Phase 3.

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Brivanib, CAS 649735-46-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 50.00
2 mg	In stock	$ 70.00
5 mg	In stock	$ 111.00
10 mg	In stock	$ 183.00
25 mg	In stock	$ 373.00
50 mg	In stock	$ 569.00
1 mL * 10 mM (in DMSO)	In stock	$ 111.00

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Description	Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3.
Targets&IC50	VEGFR2:25 nM
In vitro	Brivanib also inhibits VEGFR1 and FGFR-1 with IC50 of 0.38 μM and 0.148 μM. Brivanib is not sensitive to PDGFRβ, EGFR, LCK, PKCα or JAK-3 with IC50 all above 1900 nM. Brivanib could inhibit the proliferation of VEGF-stimulated HUVECs with IC50 of 40 nM, compared to 276 nM in FGF-stimulated HUVECs. On the other hand, Brivanib exhibits low activity to tumor cell lines. [1]
In vivo	Brivanib displays antitumor activities in H3396 xenograft in athymic mice. At a dose of 60 and 90 mg/kg (p.o.), Brivanib completely inhibits the tumor growth, with TGI of 85% and 97%, respectively. [1] Moreover, Brivanib significantly suppresses tumor growth in Hepatocellular carcinoma (HCC) xenografts, which due to the decrease in phosphorylation of VEGFR2. The results show that the tumor weights in 06-0606 xenograft mice are 55% and 13%, compared with the controls at a dose of 50 mg/kg and 100 mg/kg. Brivanib is suggested to be efficient in treatment of HCC. [2]
Kinase Assay	In Vitro Kinase Assays: Recombinant proteins containing tyrosine kinases are expressed as GST fusion proteins using baculovirus expression vector system in Sf9 cells. All enzymes are stored at -80 °C. Brivanib is dissolved in DMSO and diluted by water/10% DMSO. The VEGFR2 kinase solution is composed by 8 ng GST-VEGFR2 enzyme, 75 μg/mL substrate, 1 μM ATP, and 0.04 μCi [γ-33P]-ATP in 50 μL buffer: 20 mM Tris (pH 7.0), 25 μg/mL BSA, 1.5 mM MnCl2, 0.5 mM dithiothreitol). Flk-1 kinase solution is composed by 10 ng GST-Flk-1 enzyme, 75 μg/mL substrate, 1 μM ATP, and 0.04 μCi [γ-33P]-ATP in 50 μL buffer: 20 mM Tris, pH 7.0, 25 μg/mL BSA, 4 mM MnCl2, 0.5 mM dithiothreitol). The reactions are incubated for 1 hour at 27 °C and terminated with cold trichloroacetic acid (TCA) to a final concentration of 15%. These TCA precipitates are collected onto unifilter plates and quantitated by liquid scintillation counter.
Cell Research	The cells are stimulated by VEGF or FGF at a concentration of 8 or 80 ng/mL. These cells are seeded in 96 well plates at a density of 2 × 103 and incubated for 24 hours. Brivanib at various dilutions are added to the cells for another 48 hours. Then 0.5 μCi of [3H] thymidine is added for 24 hours. After that the incorporated tritium is quantified using a β-counter. (Only for Reference)

Synonyms	BMS-540215
Molecular Weight	370.38
Formula	C19H19FN4O3
CAS No.	649735-46-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 3 mg/mL (8.09 mM)

DMSO: 69 mg/mL (186.3 mM)

H2O: <1 mg/mL

References and Literature

1. Bhide RS, et al., J Med Chem, 2006, 49 (7), 2143-2146. 2. Huynh H, et al. Clin Cancer Res, 2008, 14(19), 6146-6153.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Drug Repurposing Compound Library Membrane Protein-targeted Compound Library Immunology/Inflammation Compound Library Bioactive Compounds Library Max Autophagy Compound Library Bioactive Compound Library

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Keywords

Brivanib 649735-46-6 Angiogenesis Autophagy JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR FGFR VEGFR inhibit BMS540215 Vascular endothelial growth factor receptor BMS 540215 BMS-540215 Inhibitor inhibitor

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