CDK inhibitor E9 ( E9 )

Catalog No. M13145 CAS No. 2020052-55-3

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Datasheet

HNMR

HPLC

MSDS

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Product Name

CDK inhibitor E9
Note

Research use only, not for human use.
Brief Description

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.
Description

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; does not serve as a substrate for either ABCB1 or ABCG2, while avoiding ABC transporter-mediated efflux; 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.
Synonyms

E9
Pathway

Angiogenesis
Target

CDK
Recptor

CDK
Research Area

——
Indication

——

CAS Number

2020052-55-3
Formula Weight

434.54
Molecular Formula

C24H30N6O2
Purity

>98% (HPLC)
Solubility

——
SMILES

C=CC(NC1=CC=CC(NC2=CC(N3[C@H](CCO)CCCC3)=NC4=C(CC)C=NN24)=C1)=O
Chemical Name

(S)-N-(3-((3-ethyl-5-(2-(2-hydroxyethyl)piperidin-1-yl)pyrazolo[1,5-a]pyrimidin-7-yl)amino)phenyl)acrylamide

1. Gao Y, et al. Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5.

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