(R)-CR8
货号：
14006-50mg 基本售价：
8250.0 元 规格：
50 mg
产品信息
概述| 货号 | 14006-50mg |
| 描述 | Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy.1 (R)-CR8 is a second-generation analog of (R)-roscovitine (Item No. 10009569) 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.2,3 (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).2,3 (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.2 |
性能| 供应商 | Cayman |
| 应用文献 |
1.Bettayeb, K.,Baunbaek, D.,Delehouze, C., et al. CDK inhibitors roscovitine and CR8 trigger Mcl-I down-regulation and apoptotic cell death in neuroblastoma cells. Genes Cancer 1(4), 369-380 (2010).
2.Bettayeb, K.,Oumata, N.,Echalier, A., et al. CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. Oncogene 27, 5797-5807 (2008).
3.Oumata, N.,Bettayeb, K.,Ferandin, Y., et al. Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1. Journal of Medicinal Chemistry 51, 5229-5242 (2008).
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| 运输条件 | Wet ice in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 431.5 |
| 分子式 | C24H29N7O |
| CAS号 | 294646-77-8 |
| 稳定性 | ≥ 2 years |
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