CDK12-IN-4
Names
[ CAS No. ]:
2651196-69-7
[ Name ]:
CDK12-IN-4
Biological Activity
[Description]:
CDK12-IN-4, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 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].
[Related Catalog]:
[Target]
CDK12:0.641 μM (IC50)
CDK2/cyclinE:>20 μM (IC50)
CDK9/cyclinT1:>20 μM (IC50)
[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 IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 581[1].
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C20H20F2N8O
[ Molecular Weight ]:
426.42