(R)-CR8
An inhibitor of cyclin-dependent kinases
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包装价格促销价数量
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1mg￥1175.00940.00- +
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10mg￥4012.003210.00- +
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50mg￥11500.009200.00- +
- 货号: ajci67674
- CAS: 294646-77-8
- 别名: (2R)-2-[[9-异丙基-6-[[[4-(2-吡啶基)苯基]甲基]氨基]-9H-嘌呤-2-基]氨基]-1-丁醇,CR8, (R)-Isomer
- 分子式: C24H29N7O
- 分子量: 431.5
- 纯度: ＞98%
- 溶解度: DMSO: Soluble,Ethanol: Soluble
- 储存: Store at -20°C
- 库存: 现货
Background
Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-CR8 is a second-generation analog of (R)-roscovitine that inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk5/p25, and Cdk9/cyclin T with IC50 values of 0.09, 0.072, 0.041, 0.11, and 0.18 μM, respectively. (R)-CR8 has 2- to 4-fold improved potency for the inhibition of CDKs over (R)-roscovitine and can inhibit the proliferation of various cancer cell lines with ~40-fold more potency than (R)-roscovitine (IC50s ~ 0.39 versus 27.8 μM, respectively). (R)-CR8 also inhibits casein kinase 1 (CK1δ/ε) with an IC50 value of 0.40 μM and inhibits GSK3α/β with an IC50 value of 12 μM.
