CDK12-IN-5

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CDK12-IN-5 

CDK12-IN-5 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 23.9 nM。CDK12-IN-5 在高 ATP (2 mM) 下对 CDK2/Cyclin E (IC50=173 μM) 和 CDK9/Cyclin T1 (IC50=127 μM) 没有影响(WO2021116178A1)。

CDK12-IN-5

CDK12-IN-5 Chemical Structure

CAS No. : 2651200-35-8

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生物活性

CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1)[1].

IC50 & Target[1]

CDK12

23.9 nM (IC50)

CDK2/cyclinE

173 μM (IC50)

CDK9/cyclinT1

127 μM (IC50)

体外研究
(In Vitro)

CDK12-IN-5 (Example 426) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=3.23 nM) and has no effect on CAL-120 cells[1].
CDK12-IN-5 has antproliferative activity in MDA-MB-231 cells (IC50=4.19 nM) and CAL-120 cells (IC50=3.57 nM)[1].
CDK12-IN-5 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 32[1].

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

454.36

Formula

C18H15F5N8O
CAS 号

2651200-35-8
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]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.

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