CDK12-IN-4

Modify Date: 2025-08-26 14:17:04

CDK12-IN-4 Structure
CDK12-IN-4 structure
Common Name CDK12-IN-4
CAS Number 2651196-69-7 Molecular Weight 426.42
Density N/A Boiling Point N/A
Molecular Formula C20H20F2N8O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of CDK12-IN-4


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].

 Names

Name CDK12-IN-4

 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

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

 Chemical & Physical Properties

Molecular Formula C20H20F2N8O
Molecular Weight 426.42
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