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PF-06726304

Chemical Structure : PF-06726304

CAS No.: 1616287-82-1

PF-06726304 (PF06726304)

Catalog No.: PC-62527Not For Human Use, Lab Use Only.

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).

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Biological Activity

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).
PF-06726304 displays very potent EZH2 biochemical inhibition as well as good activity in the cell H3K27Me3 reduction (IC50=15 nM) and antiproliferation effect.
PF-06726304 also exhibits robust in vivo antitumor growth activity and dose-dependent de-repression of EZH2 target genes.

Physicochemical Properties

M.Wt 446.328
Formula C22H21Cl2N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

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

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