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Cat. No.: HY-103682A

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PF-06726304 acetate

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

PF-06726304 acetate is a potent and selective EZH2 inhibitor. PF-06726304 acetate inhibits wild-type and Y641N mutant EZH2 with K_is 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.

CAS No.: 2080306-28-9
Formula: C₂₄H₂₅Cl₂N₃O₅
Molecular Weight:506.38

Storage:

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

Data Sheet (275 KB)

PF-06726304 acetate Chemical Structure

CAS No.: 2080306-28-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Purity & Documentation
References
Calculators
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Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

EZH2 WT

0.7 nM (Ki)

EZH2 Y641N

3.0 nM (Ki)

All Histone Methyltransferase Isoforms :

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.

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.

Chemical Information

CAS No. 2080306-28-9
Molecular Weight 506.38
Formula C₂₄H₂₅Cl₂N₃O₅
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.

Publications (1)

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Front Cell Dev Biol

EZH2/EHMT2 Histone Methyltransferases Inhibit the Transcription of DLX5 and Promote the Transformation of Myelodysplastic Syndrome to Acute Myeloid Leukemia. [Abstract]

2021 Aug 2;9:619795. PMID: 34409024

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

PF-06726304 acetate

1 Cited Publications

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Purity & Documentation
References

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PF-06726304 acetate

Publications Citing Use of MedChemExpress (MCE) PF-06726304 acetate

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Publications (1)

Purity & Documentation

References

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Help & FAQs

PF-06726304 acetate Related Classifications

HY-103682A Related Classifications