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Cdk4/6 Inhibitor IV
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。
Cdk4/6 Inhibitor IV图片
CAS NO:359886-84-3
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
GP-82996 (CINK4) 是 CDK4/6 的药理学抑制剂。 GP-82996 的 IC50 分别为 1.5、5.6 和 25 μ；M 分别代表 CDK4/cyclin D1、CDK6/cyclin D1 和 Cdk5/p35。 GP-82996 诱导癌细胞 U2OS 的凋亡。 GP-82996可用于癌症研究。
Cas No.359886-84-3
别名CINK4
化学名trans-4-[[6-(ethylamino)-2-[[1-(phenylmethyl)-1H-indol-5-yl]amino]-4-pyrimidinyl]amino]-cyclohexanol
Canonical SMILESCCNC1=NC(NC2=CC=C(N(CC3=CC=CC=C3)C=C4)C4=C2)=NC(N[C@H]5CC[C@H](O)CC5)=C1
分子式C27H32N6O
分子量456.6
溶解度≤1mg/ml in ethanol;30mg/ml in DMSO;20mg/ml in dimethyl formamide
储存条件Store at -20℃
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

Cdk4/6 inhibitor IV is a cell-permeable triaminopyrimidine inhibitor for Cdk4/cyclin D1 and Cdk6/cyclin D1 [1].

Cyclin-dependent kinase 4 (Cdk4) is an important cell cycle kinase, since its activity is required for initiating the phosphorylation of the retinoblastoma protein (pRb). Hyperphosphorylation of pRb prevents cells from initiating DNA synthesis, releases the sequestered transcription factors, leading to the loss of pRb's growth-inhibitory function, thus allowing cells to enter S phase [1].

In vitro: Cdk4/6 inhibitor IV showed an inhibitory effect on Cdk4/cyclin D1 and Cdk6/cyclin D1with the IC50 values of 1.5 and 5.6 μM, respectively. Cdk4/6 inhibitor IV exihibited potent selectivity for Cdk4/6 over Cdk5/p35, c-met, v-abl, IGF-1R, insulin receptor, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D2, Cdk6/cyclin D2, and Cdk1/cyclin B with the IC50 values ≥ 10-100 μM. In asynchronous cell lines, at 5-10 μM, Cdk4/6 inhibitor IV blocked retinoblastoma protein phosphorylation at Ser780 and Ser795, inducing cell cycle arrest in the G1 phase and apoptosis.

In vivo: In mice xenografted with human HCT116 colon carcinoma, treatment with of Cdk4/6 inhibitor IV (i.p, 30 mg/kg) after 29 days suppressed tumor growth.

Reference:
[1] Soni R, O'Reilly T, Furet P, et al.  Selective in vivo and in vitro effects of a small molecule inhibitor of cyclin-dependent kinase 4[J]. Journal of the National Cancer Institute, 2001, 93(6): 436-446.