2651200-35-8
2651200-35-8 structure
- Name: CDK12-IN-5
- Chemical Name: CDK12-IN-5
- CAS Number: 2651200-35-8
- Molecular Formula: C18H15F5N8O
- Molecular Weight: 454.36
- Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
- Create Date: 2021-11-02 19:00:17
- Modify Date: 2024-01-20 15:32:53
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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].
| Name | CDK12-IN-5 |
|---|
| 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 |
| Molecular Formula | C18H15F5N8O |
|---|---|
| Molecular Weight | 454.36 |