CDK12-IN-5

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CDK12-IN-5

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CAS NO:

2651200-35-8

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)。

生物活性

CDK12-IN-5, a pyrazolotriazine, is a potentCDK12 inhibitorwith anIC₅₀of 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 IC₅₀CDK12 high ATP to Degradation DC₅₀CDK12 ratio of 32^[1].

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.