1. Epigenetics
  2. Histone Methyltransferase
  3. PF-06726304 acetate

PF-06726304 acetate 

Cat. No.: HY-103682A
Handling Instructions

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.

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

PF-06726304 acetate Chemical Structure

PF-06726304 acetate Chemical Structure

CAS No. : 2080306-28-9

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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].

IC50 & Target[1]

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.
Molecular Weight

506.38

Formula

C₂₄H₂₅Cl₂N₃O₅

CAS No.

2080306-28-9

SMILES

O=C1N(CC2=C(C)C=C(C)NC2=O)CCC3=C1C(Cl)=C(C4=C(C)ON=C4C)C=C3Cl.CC(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

PF-06726304PF06726304PF 06726304Histone MethyltransferaseEZH2Y641NantitumorKarpas-422H3K27me3Inhibitorinhibitorinhibit

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PF-06726304 acetate
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HY-103682A
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