CDK6/9-IN-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CDK6/9-IN-1 

CDK6/9-IN-1 (compound 66) 是具有口服活性的 CDK 6 CDK 9 的双抑制剂,其对 CDK 6 CDK 9IC50 值分别为 40.5 nM 和 39.5 nM。

CDK6/9-IN-1

CDK6/9-IN-1 Chemical Structure

CAS No. : 2414373-55-8

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生物活性

CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively[1].

IC50 & Target[1]

CDK6

40.5 nM (IC50)

CDK9

39.5 nM (IC50)

体外研究
(In Vitro)

CDK6/9-IN-1 (compound 66, 4 or 8 μM in MDA-MB-231 cells) treatment induces G0/G1 cell cycle arrest (71.85% and 77.51%, respectively), when compared with the control (57.65%)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

CDK6/9-IN-1 (compound 66) significantly inhibits tumor growth in an xenograft mouse model with no obvious toxicity, indicating the promising therapeutic potential of CDK6/9 dual inhibitors for cancer treatment[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

452.94

Formula

C22H25ClN8O

CAS 号

2414373-55-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Yang Wang, et al. Discovery and SARs of 5-Chloro- N4-phenyl- N2-(pyridin-2-yl)pyrimidine-2,4-diamine Derivatives as Oral Available and Dual CDK 6 and 9 Inhibitors With Potent Antitumor Activity. J Med Chem. 2020 Mar 26;63(6):3327-3347.

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