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PF-06726304

Catalog No. T12428L   CAS 1616287-82-1

PF-06726304 shows robust antitumor growth activity. PF-06726304 is an effective and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 (Kis: 0.7 and 3.0 nM, respectively).

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PF-06726304 Chemical Structure
PF-06726304, CAS 1616287-82-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 33.00
2 mg In stock $ 46.00
5 mg In stock $ 74.00
10 mg In stock $ 127.00
25 mg In stock $ 293.00
50 mg In stock $ 531.00
100 mg In stock $ 768.00
1 mL * 10 mM (in DMSO) In stock $ 81.00
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Purity: 98.3%
Purity: 98.19%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-06726304 shows robust antitumor growth activity. PF-06726304 is an effective and selective EZH2 inhibitor. PF-06726304 inhibits wild-type and Y641N mutant EZH2 (Kis: 0.7 and 3.0 nM, respectively).
Targets&IC50 EZH2 Y641N:3.0 nM (ki), EZH2 WT:0.7 nM (ki)
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) [1].
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[1].
Molecular Weight 446.33
Formula C22H21Cl2N3O3
CAS No. 1616287-82-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 15 mg/mL (33.61 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Compound Library Chromatin Modification Compound Library Methylation Compound Library Histone Modification Compound Library Reprogramming Compound Library Bioactive Compounds Library Max Stem Cell Differentiation Compound Library Epigenetics Compound Library Bioactive Compound Library

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Keywords

PF-06726304 1616287-82-1 Chromatin/Epigenetic Histone Methyltransferase antitumor H3K27me3 Karpas-422 PF 06726304 EZH2 inhibit Inhibitor Y641N PF06726304 inhibitor

 

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