产品
编 号:F754407
分子式:C20H21F2N9
分子量:425.44
产品类型
结构图
CAS No: 2651196-71-1
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产品详情
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).
体外研究:
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. CDK12-IN-6 has antproliferative activity in MDA-MB-231 cells (IC50=2.19 nM) and CAL-120 cells (IC50=1 nM). CDK12-IN-6 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 1851.