Tazemetostat

Key Product Details

Product Description

Tazemetostat is a potent and selective EZH2 inhibitor (K_i = 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.

Product Specifications for Tazemetostat

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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	0.70 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	0.70 mL

Calculators

Background References

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

• Knutson Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2. Prc.Natl.Acad.Sci.U.S.A. 2013 PMID: 23620515
• Li EZH2 regulates neuroblastoma cell differentiation via NTRK1 promoter epigenetic modifications. Oncogene 2018 PMID: 29507419
• Li EZH2 inhibitors suppress colorectal cancer by regulating macrophage polarization in the tumor microenvironment. Front.Immunol. 2022 PMID: 35432300

Product Documents for Tazemetostat