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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 | Cdk4-CyclinD1:13.5 μM, CDK2-CyclinA:69 μM, CDK9-CyclinT1:0.35 μM, CDK2-CyclinE:20 μM, CDK1-CyclinB:44 μM, CDK7-CyclinH:26 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. | |||||||||||||||||||||||||||||||||||
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