Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 3 mg/mL (8.09 mM)
DMSO: 69 mg/mL (186.3 mM)
H2O: <1 mg/mL
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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