PF-06726304

SKU: orb1309262

Description

PF-06726304 is a potent and selective EZH2 inhibitor, effective against both wild-type and mutant Y641N forms with Kis of 0.7 nM and 3.0 nM, respectively. It demonstrates robust antitumor activity in preclinical research, making it a valuable tool for investigating epigenetics in oncology, both in vitro and in vivo.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1616287-82-1
• MW: 446.33
• Purity: 99.54% (May vary between batches)
• Formula: C₂₂H₂₁Cl₂N₃O₃
• SMILES: Cc1noc(C)c1-c1cc(Cl)c2CCN(Cc3c(C)cc(C)[nH]c3=O)C(=O)c2c1Cl
• Target: Histone Methyltransferase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.24 mM);DMSO:45 mg/mL (100.82 mM)

Bioactivity

• Target IC50:
  EZH2 (WT):0.7 nM （ki）|EZH2 (Y641N):3.0 nM （ki）
• In Vivo:
  In a subcutaneous Karpas-422 xenograft model, PF-06726304 (200 and 300 mg/kg; BID for 20 days) suppresses tumor growth and causes robust modulation of downstream biomarkers.
• In Vitro:
  PF-06726304 suppresses the proliferation of Karpas-422 cells that harbor wild-type EZH2 (IC50: 25 nM). PF-06726304 suppresses H3K27me3 in Karpas-422 (IC50: 15 nM) .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Y641N, PF 06726304, PF06726304, PF-06726304, antitumor, Inhibitor, HistoneMethyltransferase, Histone Methyltransferase, EZH2, EZH2 WT, EZH2 Y641N, H3K27me3, inhibit, Karpas-422

Compound Identifiers

PubChem CID

86723730