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CDK4 inhibitor
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CDK4 inhibitor图片
CAS NO:1256963-02-6
包装与价格:
包装价格(元)
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍

CDK4/Cyclin D1 inhibitor

Cas No.1256963-02-6
别名瑞博西尼
化学名4-(3-chloro-5-propan-2-yl-1H-pyrazol-4-yl)-N-[5-[4-(dimethylamino)piperidin-1-yl]pyridin-2-yl]pyrimidin-2-amine
Canonical SMILESCC(C)C1=C(C(=NN1)Cl)C2=NC(=NC=C2)NC3=NC=C(C=C3)N4CCC(CC4)N(C)C
分子式C22H29ClN8
分子量440.97
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 0.25 mg/ml
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

CDK4 inhibitor is a selective inhibitor of cyclin-dependent kinase 4 with IC50 value of 10 nM [1].

Cyclin-dependent kinase 4 (CDK4) is a Ser/Thr protein kinase and is a member of the cyclin-dependent kinase family. CDK4 plays an important role in the G1-S phase.

CDK4 inhibitor is a selective cyclin-dependent kinase 4 inhibitor. CDK4 inhibitor inhibited CDK4/Cyclin D1, CDK1/Cyclin B and CDK2/Cyclin A with IC50 values of 10 nM, 15 μM and 5.265 μM, respectively. Also, it inhibited protein kinase A (PKA) and glycogen synthase kinase (GSK3β) with IC50 values of 6.8 and 9.6 μM, respectively. In a mantle-cell lymphoma cell line Jeko-1, CDK4 inhibitor inhibited the phosphorylation level of pRb at the Ser780 site with IC50 value of 0.324 μM. Also, CDK4 inhibitor (0.37 μM) showed G1 block on cells [1].

Reference:
[1]. Cho YS, Borland M, Brain C, et al. 4-(Pyrazol-4-yl)-pyrimidines as selective inhibitors of cyclin-dependent kinase 4/6. J Med Chem, 2010, 53(22): 7938-7957.