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Chemical Structure : CDK12 inhibitor E9 R-isomer
Catalog No.: PC-60491Not For Human Use, Lab Use Only.
CDK12 inhibitor E9 R-isomer is a clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux.
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CDK12 inhibitor E9 R-isomer is a clinical analog of THZ1 and a selective, covalent CDK12 inhibitor that is not susceptible to ABC transporter-mediated drug efflux.
CDK12 inhibitor E9 R-isomer 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).
CDK12 inhibitor E9 R-isomer exerts its cytotoxic effects through covalent modification of cysteine 1039 of CDK12.
CDK12 inhibitor E9 R-isomer 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.
| M.Wt | 434.544 | |
| Formula | C24H30N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Gao Y, et al. Cell Chem Biol. 2017 Dec 15. pii: S2451-9456(17)30424-5.
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