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.
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
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
Keywords: PF 06726304 acetate, supplier, PF06726304, acetate, highly, potent, EZH2, inhibitors, inhibits, enhancer, of, zeste, homolog, 2, lysine, methyltransferase, PRC2, polycomb, repressive, complex, 2, Lysine, Methyltransferases, Lysine, Methyltransferases, Lysine, Methyltransferases, Tocris Bioscience