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

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.

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PF-06726304 acetate Chemical Structure

PF-06726304 acetate Chemical Structure

CAS No. : 2080306-28-9

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PF-06726304 acetate Related Antibodies

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PF-06726304 acetate Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Masse moléculaire

506.38

Formule

C24H25Cl2N3O5
CAS No.
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
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PF-06726304 acetate Related Classifications

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Keywords:

PF-067263042080306-28-9PF06726304PF 06726304Histone MethyltransferaseEZH2Y641NantitumorKarpas-422H3K27me3Inhibitorinhibitorinhibit

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