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Brivanib

Brivanib

产品编号 T6036   CAS 649735-46-6
别名: BMS-540215, 布立尼布

Brivanib (BMS-540215) 是一种针对 VEGFR2 的 ATP 竞争性抑制剂,IC50 为 25 nM。它对 VEGFR-1 和 FGFR-1 具有中等效力,对 VEGFR2 的选择性是对 PDGFR-β 的 240 倍。

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Brivanib Chemical Structure
Brivanib, CAS 649735-46-6
规格 价格/CNY 货期 数量
1 mg ¥ 457 现货
2 mg ¥ 578 现货
5 mg ¥ 913 现货
10 mg ¥ 1,580 现货
25 mg ¥ 3,130 现货
50 mg ¥ 4,590 现货
1 mL * 10 mM (in DMSO) ¥ 972 现货
其他形式的 Brivanib:
产品目录号及名称: Brivanib (T6036)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 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.
靶点活性 VEGFR2:25 nM
体外活性 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]
体内活性 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]
激酶实验 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.
细胞实验 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)
别名 BMS-540215, 布立尼布
分子量 370.38
分子式 C19H19FN4O3
CAS No. 649735-46-6

存储

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

溶解度

Ethanol: 3 mg/mL (8.09 mM)

DMSO: 69 mg/mL (186.3 mM)

H2O: <1 mg/mL

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol / DMSO 1 mM 2.6999 mL 13.4996 mL 26.9993 mL 67.4982 mL
5 mM 0.54 mL 2.6999 mL 5.3999 mL 13.4996 mL
DMSO 10 mM 0.27 mL 1.35 mL 2.6999 mL 6.7498 mL
20 mM 0.135 mL 0.675 mL 1.35 mL 3.3749 mL
50 mM 0.054 mL 0.27 mL 0.54 mL 1.35 mL
100 mM 0.027 mL 0.135 mL 0.27 mL 0.675 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

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.
PP1 Tyrosine kinase-IN-7 WHI-P154 ZM323881 hydrochloride CL-387785 BMS-599626 RG13022 Oritinib

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

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

 

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