(R)-CR8 (CR8) 是 Roscovitine 的第二代类似物,是一种有效的 CDK1/2/5/7/9 抑制剂。
Cas No. |
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 |
Canonical SMILES |
CC(C)N(C=N1)C2=C1C(NCC3=CC=C(C4=NC=CC=C4)C=C3)=NC(N[C@H](CC)CO)=N2 |
分子式 |
C24H29N7O |
分子量 |
431.5 |
溶解度 |
DMSO: Soluble,Ethanol: Soluble |
储存条件 |
Store at -20°C |
General tips |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition |
Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
半岛bd体育手机客户端 描述 |
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. |