PF 06726304 acetate

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Cat.No. 6169 - PF 06726304 acetate | C22H21Cl2N3O3.C2H4O2
Description: Highly potent and SAM-competitive EZH2 inhibitor
Chemical Name: 5,8-Dichloro-2-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-7-(3,5-dimethyl-4-isoxazolyl)-3,4-dihydro-1(2H)-isoquinolinone acetate
Purity: ≥97% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Highly potent and SAM-competitive EZH2 lysine methyltransferase inhibitor (IC50 = 0.7 nM). Inhibits proliferation of Karpas-422 cells (non-Hodgkin's lymphoma) in vitro, and halts tumor growth and reduces intratumoral H3K27Me3 levels in mice.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 506.38
Formula C22H21Cl2N3O3.C2H4O2
Storage Store at RT
Purity ≥97% (HPLC)
PubChem ID 124201861
InChI Key AVDCFFPRJKOOLX-UHFFFAOYSA-N
Smiles ClC1=C(C(N(CC2=C(C)C=C(C)NC2=O)CC3)=O)C3=C(Cl)C=C1C4=C(C)ON=C4C.CC(O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 50.64 100
ethanol 50.64 100

Preparing Stock Solutions

The following data is based on the product molecular weight 506.38. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.97 mL 9.87 mL 19.75 mL
5 mM 0.39 mL 1.97 mL 3.95 mL
10 mM 0.2 mL 0.99 mL 1.97 mL
50 mM 0.04 mL 0.2 mL 0.39 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Kung et al (2016) 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. 59 8306 PMID: 27512831


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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Epigenetics

Epigenetics Scientific Review

Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.

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