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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。
CDK12-IN-4图片
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.