PF-06726304

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-06726304 是 zeste 同源物 2 (EZH2) 抑制剂的新型强效增强剂。

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.

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.

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.

PF06726304

Chromatin/Epigenetic

HMTase

HMTase

——

——

1616287-82-1

446.328

C22H21Cl2N3O3

>98% (HPLC)

DMSO : ≥ 15 mg/mL33.61 mM

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

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

(-20℃)

With Ice Pack

≥ 2 years