Basic information Uses Safety Supplier Related
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PF-06726304 acetate

Basic information Uses Safety Supplier Related

PF-06726304 acetate Basic information

Product Name:
PF-06726304 acetate
Synonyms:
  • PF 06726304 acetate,PF06726304 acetate
CAS:
2080306-28-9
MF:
C24H25Cl2N3O5
MW:
506.38
Mol File:
2080306-28-9.mol
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PF-06726304 acetate Chemical Properties

solubility 
Soluble to 100 mM in DMSO and to 100 mM in ethanol
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PF-06726304 acetate 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].

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.

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

PF-06726304 acetateSupplier

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