2651196-69-7

2651196-69-7 structure

Name: CDK12-IN-4
Chemical Name: CDK12-IN-4
CAS Number: 2651196-69-7
Molecular Formula: C₂₀H₂₀F₂N₈O
Molecular Weight: 426.42
Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
Create Date: 2021-10-18 11:49:57
Modify Date: 2024-01-10 17:50:50
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].

Name	CDK12-IN-4

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	Research Areas >> Cancer Signaling Pathways >> Cell Cycle/DNA Damage >> CDK
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.

Molecular Formula	C₂₀H₂₀F₂N₈O
Molecular Weight	426.42