CDK12-IN-4

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CDK12-IN-4

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。

CAS NO:

2651196-69-7

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

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)。

生物活性

CDK12-IN-4, a pyrazolotriazine, is a potentCDK12 inhibitorwith anIC₅₀of 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 IC₅₀CDK12 high ATP to Degradation DC₅₀CDK12 ratio of 581^[1].

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.