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Submit ReviewPF 06726304 acetate
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)
Biological Activity for PF 06726304 acetate
PF 06726304 acetate is a 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 for PF 06726304 acetate
| M. Wt | 506.38 |
| Formula | C22H21Cl2N3O3.C2H4O2 |
| Storage | Store at RT |
| Purity | ≥97% (HPLC) |
| CAS Number | 2080306-28-9 |
| 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 for PF 06726304 acetate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 50.64 | 100 | |
| ethanol | 50.64 | 100 |
Preparing Stock Solutions for PF 06726304 acetate
The following data is based on the product molecular weight 506.38. Batch specific molecular weights may vary from batch to batch due to the degree 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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Product Datasheets for PF 06726304 acetate
References for PF 06726304 acetate
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* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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