2020052-51-9
2020052-51-9 structure
- Name: CDK12 inhibitor E9 R-isomer
- Chemical Name: CDK12 inhibitor E9 R-isomer
- CAS Number: 2020052-51-9
- Molecular Formula: C24H30N6O2
- Molecular Weight: 434.544
- Create Date: 2020-01-16 21:24:01
- Modify Date: 2024-01-18 16:47:14
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A clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux; dose-dependently decreases phosphorylated and total RNAPII in THZ1R NB and lung cancer models, competed strongly with bio-THZ1 for binding to CDK12 at low nanomolar ranges, but not CDK7 (>1 uM); exerts its cytotoxic effects through covalent modification of cysteine 1039 of CDK12; shows more potent antiproliferative activity in THZ1R NB and lung cancer cells with IC50 ranging from 8 to 40 nM than ribociclib, palbociclib, and AZD5438.
| Name | CDK12 inhibitor E9 R-isomer |
|---|
| Description | A clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux; dose-dependently decreases phosphorylated and total RNAPII in THZ1R NB and lung cancer models, competed strongly with bio-THZ1 for binding to CDK12 at low nanomolar ranges, but not CDK7 (>1 uM); exerts its cytotoxic effects through covalent modification of cysteine 1039 of CDK12; shows more potent antiproliferative activity in THZ1R NB and lung cancer cells with IC50 ranging from 8 to 40 nM than ribociclib, palbociclib, and AZD5438. |
|---|---|
| References | References 1. Gao Y, et al. Cell Chem Biol. 2017 Dec 15. pii: S2451-9456(17)30424-5. View Related Products by Target Cyclin-dependent Kinase (CDK) |
| Molecular Formula | C24H30N6O2 |
|---|---|
| Molecular Weight | 434.544 |