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Description: Potent and selective EZH2 inhibitor
Chemical Name: N-[(1,2-Dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4'-(4-morpholinylmethyl)[1,1'-biphenyl]-3-carboxamide
Purity: ≥97% (HPLC)
Biological Activity for Tazemetostat
Tazemetostat is a potent and selective EZH2 inhibitor (Ki = 2.5 nM; IC50 = 11 nM). Reduces H3K27me3 levels in PDX derived cells and inhibits cellular H3K27 methylation. Tazemetostat suppresses EZH2 and MYC expression and induces neuronal differentiation genes; also increases neurite extension in MB-39-nu cells. Antiproliferative in SMARCAB1-deleted MRT cell lines (IC50 = 32 - 1000 nM); inhibits methylation in both mutant and wild type cells (IC50 = 1.4-4.9 nM). Dose-dependently suppresses growth of both MC38 cells and tumors in vivo.
Technical Data for Tazemetostat
| M. Wt | 572.74 |
| Formula | C34H44N4O4 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 1403254-99-8 |
| PubChem ID | 66558664 |
| InChI Key | NSQSAUGJQHDYNO-UHFFFAOYSA-N |
| Smiles | O=C(NCC=1C(=O)NC(=CC1C)C)C2=CC(=CC(=C2C)N(CC)C3CCOCC3)C4=CC=C(C=C4)CN5CCOCC5 |
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 Tazemetostat
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 28.64 | 50 |
Preparing Stock Solutions for Tazemetostat
The following data is based on the product molecular weight 572.74. 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 |
|---|---|---|---|
| 0.5 mM | 3.49 mL | 17.46 mL | 34.92 mL |
| 2.5 mM | 0.7 mL | 3.49 mL | 6.98 mL |
| 5 mM | 0.35 mL | 1.75 mL | 3.49 mL |
| 25 mM | 0.07 mL | 0.35 mL | 0.7 mL |
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Product Datasheets for Tazemetostat
References for Tazemetostat
References are publications that support the biological activity of the product.
Li et al (2022) EZH2 inhibitors suppress colorectal cancer by regulating macrophage polarization in the tumor microenvironment. Front.Immunol. 13 857808 PMID: 35432300
Knutson et al (2013) Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Prc.Natl.Acad.Sci.U.S.A. 110 7922 PMID: 23620515
Li et al (2018) EZH2 regulates neuroblastoma cell differentiation via NTRK1 promoter epigenetic modifications. Oncogene 37 2714 PMID: 29507419
If you know of a relevant reference for Tazemetostat, please let us know.
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Keywords: Tazemetostat, Tazemetostat supplier, EPZ6438, EPZ-6438, EZH2, enhancer, of, zeste, homolog, potent, selective, inhibitor, inhibitors, inhibits, H3K27, neuronal, differentiation, neurite, antiproliferative, Neural, Stem, Cells, 8093, Tocris Bioscience
Citations for Tazemetostat
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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.
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 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.
Cancer Metabolism Poster
This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.
Epigenetics in Cancer Poster
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 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.