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Chemical Structure : CDK inhibitor E9
CAS No.: 2020052-55-3
Catalog No.: PC-63235Not For Human Use, Lab Use Only.
CDK inhibitor E9 is a novel CDK inhibitor that can overcomes ABC-mediated resistance of THZ1, functions as a potent, non-covalent inhibitor of CDK9 and a covalent inhibitor of CDK12.
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|---|---|---|---|
| 5 mg | $348 | In stock | |
| 10 mg | $548 | In stock | |
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CDK inhibitor E9 is a novel CDK inhibitor that can overcomes ABC-mediated resistance of THZ1, functions as a potent, non-covalent inhibitor of CDK9 and a covalent inhibitor of CDK12.
CDK inhibitor E9 does not serve as a substrate for either ABCB1 or ABCG2, while avoiding ABC transporter-mediated efflux.
CDK inhibitor E9 decreases the phosphorylated and total RNAPII in THZ1R NB and lung cancer cells (IC50=8-40 nM), accompanied by decreased MYC and MCL1 expression, exerts its cytotoxic effects through covalent modification of cysteine 1039 of CDK12.
| M.Wt | 434.544 | |
| Formula | C24H30N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(S)-N-(3-((3-ethyl-5-(2-(2-hydroxyethyl)piperidin-1-yl)pyrazolo[1,5-a]pyrimidin-7-yl)amino)phenyl)acrylamide |
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1. Gao Y, et al. Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5.
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