CDK12-IN-6

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-6 

CDK12-IN-6 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 1.19 μM。CDK12-IN-6 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-6

CDK12-IN-6 Chemical Structure

CAS No. : 2651196-71-1

规格 是否有货
5 mg 询价
10 mg 询价
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

生物活性

CDK12-IN-6, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 1.19 μM at high ATP (2 mM). CDK12-IN-6 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

1.19 μM (IC50)

CDK2/cyclinE

>20 μM (IC50)

CDK9/cyclinT1

>20 μM (IC50)

体外研究
(In Vitro)

CDK12-IN-6 (Example 174) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=0.872 nM) and has no effect on CAL-120 cells[1].
CDK12-IN-6 has antproliferative activity in MDA-MB-231 cells (IC50=2.19 nM) and CAL-120 cells (IC50=1 nM)[1].
CDK12-IN-6 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 1851[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

425.44

Formula

C20H21F2N9

CAS 号

2651196-71-1

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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

发表评论