CDK12-IN-5
Names
[ CAS No. ]:
2651200-35-8
[ Name ]:
CDK12-IN-5
Biological Activity
[Description]:
CDK12-IN-5, a pyrazolotriazine, is a potent CDK12 inhibitor with an IC50 of 23.9 nM at high ATP (2 mM). CDK12-IN-5 has no effect on CDK2/Cyclin E (IC50=173 μM) and CDK9/Cyclin T1 (IC50=127 μM) at high ATP (2 mM) (WO2021116178A1)[1].
[Related Catalog]:
[Target]
CDK12:23.9 nM (IC50)
CDK2/cyclinE:173 μM (IC50)
CDK9/cyclinT1:127 μM (IC50)
[In Vitro]
CDK12-IN-5 (Example 426) inhibits BRCA1 MRNA expression in MDA-MB-231 cells (IC50=3.23 nM) and has no effect on CAL-120 cells[1]. CDK12-IN-5 has antproliferative activity in MDA-MB-231 cells (IC50=4.19 nM) and CAL-120 cells (IC50=3.57 nM)[1]. CDK12-IN-5 has a inhibition IC50 CDK12 high ATP to Degradation DC50 CDK12 ratio of 32[1].
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C18H15F5N8O
[ Molecular Weight ]:
454.36