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.
In Vitro

PF-06726304 (Compound 31) inhibits H3K27me3 in Karpas-422 with an IC50 of 15 nM.PF-06726304 inhibits the proliferation of Karpas-422 cells that harbor wild-type EZH2 with an IC50 of 25 nM.
In Vivo

PF-06726304 (200 and 300 mg/kg; BID for 20 days) inhibits tumor growth and induces robust modulation of downstream biomarkers in a subcutaneous Karpas-422 xenograft model. Animal Model:Female Scid beige mice (6-8 weeks old) with Karpas-422 xenograft model Dosage:200 and 300 mg/kg Administration:Given BID for 20 days Result:Inhibited tumor growth and induced robust modulation of downstream biomarkers in a subcutaneous Karpas-422 xenograft model.
Synonyms

PF06726304
Pathway

Chromatin/Epigenetic
Target

HMTase
Recptor

HMTase
Research Area

——
Indication

——

CAS Number

1616287-82-1
Formula Weight

446.328
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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