Powder: -20°C for 3 years | In solvent: -80°C for 1 year
EPZ015666 (GSK3235025) 是一种口服有效的 PRMT5 酶活性抑制剂,IC50为 22 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 587 | 现货 | ||
5 mg | ¥ 943 | 现货 | ||
10 mg | ¥ 1,541 | 现货 | ||
25 mg | ¥ 3,666 | 现货 | ||
50 mg | ¥ 3,990 | 现货 | ||
100 mg | ¥ 5,830 | 现货 | ||
200 mg | ¥ 8,090 | 现货 | ||
500 mg | ¥ 11,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 995 | 现货 |
产品描述 | EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity. |
靶点活性 | PRMT5:5 nM(Ki) |
体外活性 | 口服200 mg/kg EPZ015666对MCL异种移植动物模型具有强的抗肿瘤活性. |
体内活性 | EPZ015666显示有效的细胞活性,阻断SmD3的对称二甲基化,并抑制MCL细胞系的增殖,IC50为96-904 nM。 |
激酶实验 | EPZ015666 is serially diluted threefold from 1,000 to 0.051 nM and spotted into a 384-well polypropylene V-bottom microplate. 3H-SAM is serially diluted twofold in assay buffer for a seven-point dilution series with a top concentration of 700 nM (final assay concentration). Reactions are initiated by the addition of 4 nM enzyme and 40 nM peptide (final assay concentrations for both). Reactions are incubated for 60 min and quenched by the addition of 10 μL per well of 600 μM unlabeled SAM in assay buffer (final assay concentration). For the peptide competition, EPZ015666 is serially diluted threefold from 1,000 to 0.051 nM and spotted into a 384-well polypropylene V-bottom microplate. Peptide is serially diluted twofold in assay buffer for a seven-point dilution series with a top concentration of 480 nM (final assay concentration). Reactions are initiated by the addition of 4 nM enzyme and 75 nM 3H-SAM (final assay concentrations for both). Reactions are incubated for 60 min, and the reactions are quenched by the addition of 10 μL per well of 600 μM unlabeled SAM in assay buffer (final assay concentration)[1]. |
细胞实验 | EPZ015666 is dissolved in DMSO and stored, and then diluted with appropriate medium (final DMSO 0.2%) before use[1]. Cultured cells in linear/log-phase growth are split to a seeding density of 2×105 cells/mL in 2-20 mL of media, depending on the yield required at the end of the growth period. Compound is diluted in DMSO and added to each culture vessel with a final DMSO concentration of 0.2%. Cells are allowed to grow for 96 h undisturbed. At the conclusion of each treatment period, cells are harvested by centrifugation (5 min, 1,200 rpm), and cell pellets are rinsed once with PBS before being frozen on dry ice pending further processing. Long-term proliferation assays are performed on all MCL lines, with slight adjustments to initial seeding densities, depending on growth characteristics for each cell line. All assays are carried out for 12 d[1]. |
别名 | GSK3235025 |
化合物与蛋白结合的复合物 |
Crystal structure of PRMT5:MEP50 with EPZ015666 and sinefungin |
分子量 | 383.44 |
分子式 | C20H25N5O3 |
CAS No. | 1616391-65-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 56 mg/mL (146 mM)
Ethanol: 45 mg/mL (117.4 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.608 mL | 13.0398 mL | 26.0797 mL | 65.1992 mL |
5 mM | 0.5216 mL | 2.608 mL | 5.2159 mL | 13.0398 mL | |
10 mM | 0.2608 mL | 1.304 mL | 2.608 mL | 6.5199 mL | |
20 mM | 0.1304 mL | 0.652 mL | 1.304 mL | 3.26 mL | |
50 mM | 0.0522 mL | 0.2608 mL | 0.5216 mL | 1.304 mL | |
100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.652 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。
EPZ015666 1616391-65-1 Chromatin/Epigenetic Histone Methyltransferase inhibit Inhibitor GSK-3235025 EPZ 015666 EPZ-015666 GSK 3235025 GSK3235025 inhibitor