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CAN508 是一种有效的 ATP 竞争性 CDK9/cyclin T1 抑制剂,IC50 为 0.35 μM。它还是 Cdk2-cyclin E 对 ATP 的竞争性抑制剂,Ki 和 IC50 值分别为 13.3 和 20 µM。它对 CDK9/cyclin T 的选择性是其他 CDK/cyclin 复合物的 38 倍,有抗肿瘤活性。
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CAN508 是一种有效的 ATP 竞争性 CDK9/cyclin T1 抑制剂,IC50 为 0.35 μM。它还是 Cdk2-cyclin E 对 ATP 的竞争性抑制剂,Ki 和 IC50 值分别为 13.3 和 20 µM。它对 CDK9/cyclin T 的选择性是其他 CDK/cyclin 复合物的 38 倍,有抗肿瘤活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 108 | In stock | |
5 mg | ¥ 209 | In stock | |
10 mg | ¥ 313 | In stock | |
25 mg | ¥ 625 | In stock | |
50 mg | ¥ 931 | In stock | |
100 mg | ¥ 1,390 | In stock | |
200 mg | ¥ 1,980 | In stock | |
1 mL x 10 mM (in DMSO) | ¥ 251 | In stock |
CAN508 相关产品
产品描述 | CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. It is also a competitive inhibitor of Cdk2-cyclin E with respect to ATP, with Ki and IC50 values of 13.3 and 20 μM, respectively.CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity. |
靶点活性 | CDK7-CyclinH:26 μM, CDK2/cyclinE:20 μM, CDK9-CyclinT1:0.35 μM, CDK2-CyclinA:69 μM, Cdk4/cyclin D1:13.5 μM, CDK1-CyclinB:44 μM |
体外活性 | The most potent inhibitor,CAN508, reduced the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays.?Further observed cellular effects included decreased phosphorylation of the retinoblastoma protein and the C-terminal domain of RNA polymerase II, inhibition of mRNA synthesis, and induction of the tumor suppressor protein p53, all of which are consistent with inhibition of CDK9. |
分子量 | 218.22 |
分子式 | C9H10N6O |
CAS No. | 140651-18-9 |
Smiles | Nc1n[nH]c(N)c1\N=N\c1ccc(O)cc1 |
密度 | 1.67 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 250 mg/mL (1145.63 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
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