Soluble to 100 mM in DMSO and to 100 mM in ethanol
Usage And Synthesis
Uses
PF 06726304 Acetate is a useful research chemical.
Uses
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].
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].
Inhibited tumor growth and induced robust modulation of downstream biomarkers in a subcutaneous Karpas-422 xenograft model.
IC 50
EZH2 WT: 0.7 nM (Ki); EZH2 Y641N: 3.0 nM (Ki)
storage
Store at RT
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. DOI:10.1021/acs.jmedchem.6b00515
