Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and non-covalent CDK9 inhibitor while avoiding ABC transporter-mediated efflux. It has a weak binding ability to CDK7/CyclinH complex (IC50< 1 μM).
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 2,210 | 5日内发货 | ||
5 mg | ¥ 3,320 | 5日内发货 | ||
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 3,660 | 5日内发货 |
产品描述 | CDK12-IN-E9 is a potent and selective covalent CDK12 inhibitor and non-covalent CDK9 inhibitor while avoiding ABC transporter-mediated efflux. It has a weak binding ability to CDK7/CyclinH complex (IC50> 1 μM). |
靶点活性 | CDK2-CyclinA:932 nM, CDK7-CyclinH-MNAT1:1210 nM, CDK9-CyclinT1:23.9 nM |
体外活性 | CDK12-IN-E9 (E9; 0-3000 nM; 6 hours; Kelly, PC-9, and NCI-H82 cells) treatment leads to a dose-dependent decrease in phosphorylated and total RNAPII in THZ1r NB and lung cancer models, accompanied by decreased MYC and MCL1 expression. CDK12-IN-E9 (E9; 10 nM-10 μM; 72 hours; Kelly, LAN5, PC-9, SK-N-BE2, NCI-H82 and NCI-H3122 cells) treatment shows potent antiproliferative activity in THZ1R NB and lung cancer cells (IC50s: 8 to 40 nM). CDK12-IN-E9 also results in increased PARP cleavage, and an increase in the subGI population in THZ1r lung cancer cells, while in NB cells, more of a G2/M arrest is seen after a 24-hr exposure to CDK12-IN-E9. |
分子量 | 434.53 |
分子式 | C24H30N6O2 |
CAS No. | 2020052-55-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
CDK12-IN-E9 2020052-55-3 Cell Cycle/Checkpoint CDK CDK-12-IN-E9 CDK12INE9 CDK12 IN E9 Inhibitor inhibitor inhibit