1. Epigenetics
  2. Epigenetic Reader Domain
    Histone Methyltransferase
  3. PF-06821497

PF-06821497 

Cat. No.: HY-101571A
Handling Instructions

PF-06821497 (compound 23a) is a potent, selective, orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition.

For research use only. We do not sell to patients.

PF-06821497 Chemical Structure

PF-06821497 Chemical Structure

CAS No. : 1844849-10-0

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Description

PF-06821497 (compound 23a) is a potent, selective, orally active Enhancer of Zeste Homolog 2 (EZH2) inhibitor, with a Ki value <0.1 nM against mutant Y641N EZH2. Exhibits robust tumor growth inhibition[1].

IC50 & Target

Ki: <0.1 nM (Y641N EZH2)[1].

In Vivo

PF-06821497 (compound 23a: 100 mg/kg, PO twice daily for 31 days) treatment results in significant inhibition of tumor growth, and the the tumor regressition effect can be sustained for another 40 days after the terminal administration[1].
PF-06821497 with the dose of 300 mg/kg has minimal impact on animal body weights[1].

Animal Model: Mice bearing Karpas-422 DLBCL tumor xenografts (which contain the Y641N EZH2 mutation)[1].
Dosage: 100 mg/kg and 300 mg/kg.
Administration: PO twice daily for 31 days.
Result: 100 mg/kg dose resulted in significant inhibition of tumor growth and 300 mg/kg dose minimal effected animal body weights.
References
Molecular Weight

467.34

Formula

C₂₂H₂₄Cl₂N₂O₅

CAS No.

1844849-10-0

SMILES

COC1=C(CN2CCC(C(Cl)=CC([[email protected]](OC)C3COC3)=C4Cl)=C4C2=O)C(NC(C)=C1)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PF-06821497
Cat. No.:
HY-101571A
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PF-06821497

Cat. No.: HY-101571A