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
Reviews
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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.

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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References

References are publications that support the biological activity of the product.

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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Citations for PF 06726304 acetate

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


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.

Stem Cells

Stem Cells Scientific Review

Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.

Epigenetics

Epigenetics Research Bulletin

Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:

  • Bromodomains
  • DNA Methyltransferases
  • Histone Deacetylases
  • Histone Demethylases
  • Histone Methyltransferases
Cancer Metabolism

Cancer Metabolism Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.

Epigenetics in Cancer

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Stem Cells

Stem Cells Poster

Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.