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说明： Potent and selective EZH2 inhibitor
化学名： 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
纯度： ≥97% (HPLC)
生物活性 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.
技术数据 for Tazemetostat
| 分子量 | 572.74 |
| 公式 | C34H44N4O4 |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Tazemetostat
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 28.64 | 50 |
制备储备液 for Tazemetostat
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for Tazemetostat
参考文献 for Tazemetostat
参考文献是支持产品生物活性的出版物。
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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关键词: 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
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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.