PF-06726304 acetate

Modify Date: 2024-01-09 23:56:47

PF-06726304 acetate Structure
PF-06726304 acetate structure
Common Name PF-06726304 acetate
CAS Number 2080306-28-9 Molecular Weight 506.38
Density N/A Boiling Point N/A
Molecular Formula C24H25Cl2N3O5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of PF-06726304 acetate


PF-06726304 acetate is a potent and selective EZH2 inhibitor. PF-06726304 acetate inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 acetate displays robust antitumor growth activity[1].

 Names

Name PF-06726304 acetate

 PF-06726304 acetate Biological Activity

Description PF-06726304 acetate is a potent and selective EZH2 inhibitor. PF-06726304 acetate inhibits wild-type and Y641N mutant EZH2 with Kis of 0.7 and 3.0 nM, respectively. PF-06726304 acetate displays robust antitumor growth activity[1].
Related Catalog
Target

EZH2 WT:0.7 nM (Ki)

EZH2 Y641N:3.0 nM (Ki)

In Vitro PF-06726304 (Compound 31) inhibits H3K27me3 in Karpas-422 with an IC50 of 15 nM[1]. PF-06726304 inhibits the proliferation of Karpas-422 cells that harbor wild-type EZH2 with an IC50 of 25 nM[1].
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[1]. Animal Model: Female Scid beige mice (6-8 weeks old) with Karpas-422 xenograft model[1] 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.
References

[1]. Kung PP, et al. Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors. J Med Chem. 2016 Sep 22;59(18):8306-25.

 Chemical & Physical Properties

Molecular Formula C24H25Cl2N3O5
Molecular Weight 506.38