CDK12-IN-5

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].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

CDK12:23.9 nM (IC50)

CDK2/cyclinE:173 μM (IC50)

CDK9/cyclinT1:127 μM (IC50)

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].

[1]. Kai Thede, et al. Pyrazolotriazines. WO2021116178A1.