CDK12-IN-6
Names
[ CAS No. ]:
2651196-71-1
[ Name ]:
CDK12-IN-6
Biological Activity
[Description]:
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].
[Related Catalog]:
[Target]
CDK12:1.19 μM (IC50)
CDK2/cyclinE:>20 μM (IC50)
CDK9/cyclinT1:>20 μM (IC50)
[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].
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C20H21F2N9
[ Molecular Weight ]:
425.44