CDK12 inhibitor E9 R-isomer
Modify Date: 2025-08-25 19:22:51
CDK12 inhibitor E9 R-isomer structure
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Common Name | CDK12 inhibitor E9 R-isomer | ||
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| CAS Number | 2020052-51-9 | Molecular Weight | 434.544 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C24H30N6O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of CDK12 inhibitor E9 R-isomerA 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 |
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| 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. |
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| 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 |