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
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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 | |
| 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 |
| Molecular Formula | C20H20F2N8O |
|---|---|
| Molecular Weight | 426.42 |