CDK12-IN-4

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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。

CDK12-IN-4 

CDK12-IN-4 是一种吡唑并三嗪，是有效的 CDK12 抑制剂，在高 ATP (2 mM) 下的 IC50 为 0.641 μM。CDK12-IN-4 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50>20 μM) 和 CDK9/Cyclin T1 (IC50>20 μM) 没有影响(WO2021116178A1)。

CDK12-IN-4

CDK12-IN-4 Chemical Structure

CAS No. : 2651196-69-7

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生物活性

CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 0.641 μM at high ATP (2 mM). CDK12-IN-4 has no effect on CDK2/Cyclin E (IC50>20 μM) and CDK9/Cyclin T1 (IC50>20 μM) at high ATP (2 mM) (WO2021116178A1)[1].

IC50 & Target[1]

CDK12

0.641 μM (IC50)

CDK2/cyclinE

>20 μM (IC50)

CDK9/cyclinT1

>20 μM (IC50)

体外研究
(In Vitro)

CDK12-IN-4 (Example 172) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.626 nM) and has no effect on CAL-120 cells[1].
CDK12-IN-4 has antproliferative activity in MDA-MB-231 cells (IC50=0.535 nM) and CAL-120 cells (IC50=2.43 nM)[1].
CDK12-IN-4 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 581[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

426.42

Formula

C20H20F2N8O
CAS 号

2651196-69-7
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]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.

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