PF-06726304 ( PF06726304 )

Catalog No. M12356 CAS No. 1616287-82-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

PF-06726304
Note

Research use only, not for human use.
Brief Description

PF-06726304 is a novel potent enhancer of zeste homolog 2 (EZH2) inhibitor.
Description

PF-06726304 is a novel potent enhancer of zeste homolog 2 (EZH2) inhibitor with IC50 of <5 nM, Ki of 0.7/3.0 nM (Wt/Y641N); displays very potent EZH2 biochemical inhibition as well as good activity in the cell H3K27Me3 reduction (IC50=15 nM) and antiproliferation effect; also exhibits robust in vivo antitumor growth activity and dose-dependent de-repression of EZH2 target genes.
Synonyms

PF06726304
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

HMTase
Research Area

——
Indication

——

CAS Number

1616287-82-1
Formula Weight

446.33
Molecular Formula

C22H21Cl2N3O3
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 15 mg/mL33.61 mM
SMILES

O=C1N(CC2=C(C)C=C(C)NC2=O)CCC3=C1C(Cl)=C(C4=C(C)ON=C4C)C=C3Cl
Chemical Name

5,8-dichloro-2-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-7-(3,5-dimethylisoxazol-4-yl)-3,4-dihydroisoquinolin-1(2H)-one

1. Kung PP, et al. J Med Chem. 2016 Sep 22;59(18):8306-25.

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