Tazemetostat

Name: Tazemetostat
Brand: Tocris Bioscience
SKU: 8093

Tocris Bioscience, part of Bio-Techne | Catalog # 8093

COA / SDS

Potent and selective EZH2 inhibitor

Key Product Details

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)
Molecular Weight:	572.74

View Full Technical Details for Tazemetostat

Technical Data
Citations

Biological Activity for Tazemetostat

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.

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 for Tazemetostat

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	0.70 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

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References for Tazemetostat

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