Powder: -20°C for 3 years | In solvent: -80°C for 1 year
(S)-crizotinib (ent-crizotinib) 是一种选择性MTH1(mutT 同源物)抑制剂,IC50为 330 nM。它通过抑制 MTH1 破坏核苷酸库的稳态,诱导 DNA 单链断裂的增加,激活人结肠癌细胞的 DNA 修复,在动物模型中抑制肿瘤生长。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
2 mg | ¥ 297 | 现货 | ||
5 mg | ¥ 496 | 现货 | ||
10 mg | ¥ 745 | 现货 | ||
25 mg | ¥ 1,230 | 现货 | ||
50 mg | ¥ 1,820 | 现货 | ||
100 mg | ¥ 2,880 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 546 | 现货 |
产品描述 | (S)-crizotinib (ent-crizotinib) (IC50 of 72 nM), an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib. |
靶点活性 | MTH1:72 nM |
体外活性 | 在SW480 结肠癌模型中,每天口服 50?mg/kg(S)-Crizotinib能够阻碍肿瘤的生长. |
体内活性 | (S)-crizotinib能够激活人结肠癌细胞中DNA修复机制,它抑制MTH1从而破坏核苷酸库的稳态,进一步诱导DNA单链断裂的增加。 |
激酶实验 | MTH1 catalytic assay: Half-maximal inhibitory concentrations (IC50) are determined using a luminescence-based assay with some minor modifications. Briefly, serial dilutions of compounds are dissolved in assay buffer (100?mM Tris-acetate pH?7.5, 40?mM NaCl and 10?mM Mg(OAc)2 containing 0.005% Tween-20 and 2?mM dithiothreitol (DTT). Upon addition of MTH1 recombinant protein (final concentration 2?nM), plates are incubated on a plate shaker for 15?min at room temperature. After addition of the substrate dGTP (final concentration 100?μM), 8-oxo-dGTP (final concentration 13.2?μM), or 2-OH-dATP (final concentration 8.3?μM) the generation of pyrophosphate (PPi) as a result of nucleotide triphosphate hydrolysis by MTH1 is monitored over a time course of 15?min using the PPi Light Inorganic Pyrophosphate Assay kit. IC50 values are determined by fitting a dose-response curve to the data points using nonlinear regression analysis using the GraphPad Prism software. |
细胞实验 | One day before treatment, cells are seeded per well in six-well plates and incubated for 24 h. The next day DMSO (equal to highest amount of compound dilution, maximum 0.2%) or compounds in increasing concentrations were added and cells incubated at 37 °C, 5% CO2, for 7-10 days. After washing with PBS, cells are fixed with ice-cold methanol, stained with crystal violet solution (0.5% in 25% methanol) and left to dry overnight. For quantification of results, ultraviolet absorbance of crystal violet is determined at 595 nm following solubilisation by 70% ethanol. Data are analysed using nonlinear regression analysis using the GraphPad Prism software. (Only for Reference) |
别名 | ent-crizotinib |
分子量 | 450.34 |
分子式 | C21H22Cl2FN5O |
CAS No. | 1374356-45-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
1eq. HCl: 9 mg/mL (20 mM)), Heating is recommended.
DMSO: 22.5 mg/mL (50 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
1eq. HCl / DMSO | 1 mM | 2.2205 mL | 11.1027 mL | 22.2054 mL | 55.5136 mL |
5 mM | 0.4441 mL | 2.2205 mL | 4.4411 mL | 11.1027 mL | |
10 mM | 0.2221 mL | 1.1103 mL | 2.2205 mL | 5.5514 mL | |
20 mM | 0.111 mL | 0.5551 mL | 1.1103 mL | 2.7757 mL | |
DMSO | 50 mM | 0.0444 mL | 0.2221 mL | 0.4441 mL | 1.1103 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。
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