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Brivanib

Brivanib
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Purity:98.87%
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Brivanib

Catalog No. T6036Cas No. 649735-46-6
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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Pack SizePriceAvailabilityQuantity
1 mg$50In Stock
2 mg$70In Stock
5 mg$111In Stock
10 mg$183In Stock
25 mg$373In Stock
50 mg$569In Stock
1 mL x 10 mM (in DMSO)$111In Stock
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Product Introduction

Bioactivity
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.
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)
AliasBMS-540215
Chemical Properties
Molecular Weight370.38
FormulaC19H19FN4O3
Cas No.649735-46-6
Storage & Solubility Information
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
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM2.6999 mL13.4996 mL26.9993 mL134.9965 mL
5 mM0.5400 mL2.6999 mL5.3999 mL26.9993 mL
DMSO
1mg5mg10mg50mg
10 mM0.2700 mL1.3500 mL2.6999 mL13.4996 mL
20 mM0.1350 mL0.6750 mL1.3500 mL6.7498 mL
50 mM0.0540 mL0.2700 mL0.5400 mL2.6999 mL
100 mM0.0270 mL0.1350 mL0.2700 mL1.3500 mL

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