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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).
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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 | 库存 | 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 x 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 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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