CDK12-IN-6

Name: CDK12-IN-6
Brand: TargetMol
SKU: T40289
Rating: 4.5 (1 reviews)

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产品编号 T40289Cas号 2651196-71-1

别名 CDK12-IN-6

CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1).

CDK12-IN-6

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产品编号 T40289 别名 CDK12-IN-6Cas号 2651196-71-1

规格	价格	库存	数量
25 mg	¥ 10,600	6-8周

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产品描述	CDK12-IN-6, a pyrazolotriazine compound, is a powerful inhibitor of CDK12. Its inhibitory activity is significant with an IC50 value of 1.19 μM when tested at high ATP concentration (2 mM). Notably, CDK12-IN-6 does not exhibit any inhibitory effect on CDK2/Cyclin E (IC50 >20 μM) and CDK9/Cyclin T1 (IC50 >20 μM) when tested under the same high ATP conditions (2 mM) (WO2021116178A1).
靶点活性	CDK12:1.19 μM (IC50), CDK2-CyclinE:>20 μM (IC50), CDK9-CyclinT1:>20 μM (IC50)
体外活性	CDK12-IN-6 (Example 174) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC 50 =0.872 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-6 has antproliferative activity in MDA-MB-231 cells (IC 50 =2.19 nM) and CAL-120 cells (IC 50 =1 nM)[1]. CDK12-IN-6 has a inhibition IC 50 CDK12 high ATP to Degradation DC 50 CDK12 ratio of 1851[1].
别名	CDK12-IN-6