Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BQU57 能够选择性抑制 Ral,且对 Ral 的选择性高于 Ras、Rho,能够作用于 H2122(IC50:2.0 μM)和 H358(IC50:1.3 μM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 541 | 现货 | ||
10 mg | ¥ 932 | 现货 | ||
50 mg | ¥ 1,995 | 现货 | ||
100 mg | ¥ 3,717 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 598 | 现货 |
产品描述 | BQU57 shows selective inhibition for Ral relative to Ras or Rho and inhibit xenograft tumor growth. |
体外活性 | 50 mg/kg,i.p. BQU57在负荷人肺H2122肿瘤的小鼠体内,明显抑制RalA和RalB的活化,并且剂量依赖性抑制肿瘤生长. |
体内活性 | BQU57抑制H2122和H358细胞系中RalA与RalB活化,从而引起细胞生长抑制。 |
激酶实验 | HDAC Enzyme Assay: The commercially availablae human recombinant enzyme and fluorogenic HDAC assay kits have used to measure percent inhibition and IC50 values of three HDAC isozymes (HDAC2, HDAC4, HDAC6). Briefly, the inhibitor is added sequentially to a black, flat-bottom 96-well microtiter plate, and the reaction mixture is incubated for 30 min at 37°C. The potent HDAC inhibitor trichostatin A (included in the assay kit) is added to the bifunctional HDAC assay developer at a final reaction concentration of 1 μM to stop deacetylation and initiate the release of the fluorophore. The reaction mixture is further incubated at room temperature for 15 min. Fluorescence is measured on a Spectra Max Gemini XPS using an excitation wavelength of 360 nm and a detection wavelength of 460 nm. |
细胞实验 | Growth inhibition on human lung cancer cells by the compounds are measured under anchorage-independent conditions in soft agar. Cells are seeded into 6-well plates (coated with a base layer made of 2.0 mL of 1% low-melting-point agarose) at 15,000 cells per well in 3.0 mL of 0.4% low-melting-point agarose containing various concentration of drug. Two to four weeks (depending on cell line) after incubation, cells are stained with 1.0 mg/mL Nitro Blue Tetrazolium and colonies are counted under a microscope. The IC50 values are defined as the concentration of drug that resulted in 50% reduction in colony number compared to DMSO treated control. After 48 hr, cells are subjected to the soft agar colony formation assay. (Only for Reference) |
分子量 | 334.3 |
分子式 | C16H13F3N4O |
CAS No. | 1637739-82-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 16 mg/mL (47.9 mM)
DMSO: 61 mg/mL (182.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.9913 mL | 14.9566 mL | 29.9133 mL | 74.7831 mL |
5 mM | 0.5983 mL | 2.9913 mL | 5.9827 mL | 14.9566 mL | |
10 mM | 0.2991 mL | 1.4957 mL | 2.9913 mL | 7.4783 mL | |
20 mM | 0.1496 mL | 0.7478 mL | 1.4957 mL | 3.7392 mL | |
DMSO | 50 mM | 0.0598 mL | 0.2991 mL | 0.5983 mL | 1.4957 mL |
100 mM | 0.0299 mL | 0.1496 mL | 0.2991 mL | 0.7478 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。
BQU57 1637739-82-2 GPCR/G Protein MAPK GTPase Ras inhibit BQU 57 Inhibitor BQU-57 inhibitor