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2020052-41-7

2020052-41-7 structure
2020052-41-7 structure
  • Name: CDK12 inhibitor E9 racemate
  • Chemical Name: CDK12 inhibitor E9 racemate
  • CAS Number: 2020052-41-7
  • Molecular Formula: C24H30N6O2
  • Molecular Weight: 434.544
  • Create Date: 2020-01-20 13:45:55
  • Modify Date: 2024-01-13 19:41:45
  • 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 racemate
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