Home Tools

Tazemetostat

Catalog No. T1788 CAS 1403254-99-8

Synonyms: E-7438, EPZ6438

Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epithelioid sarcoma/follicular lymphoma.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Tazemetostat, CAS 1403254-99-8

Pack Size	Availability	Price/USD
5 mg	In stock	$ 59.00
10 mg	In stock	$ 81.00
50 mg	In stock	$ 113.00
100 mg	In stock	$ 176.00
200 mg	In stock	$ 266.00
500 mg	In stock	$ 497.00
1 mL * 10 mM (in DMSO)	In stock	$ 73.00

Bulk Inquiry

Select Batch

Purity: 99.82%

Purity: 99.72%

Purity: 99.48%

Purity: 99.38%

Purity: 98.73%

Purity: 98.66%

Purity: 98.24%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Tazemetostat (EPZ6438) is a histone methyltransferase EZH2 inhibitor (IC50=11 nM) that is orally active, selective, and SAM-competitive. Tazemetostat exhibits antitumor activity and may be used for the treatment of epithelioid sarcoma/follicular lymphoma.
Targets&IC50	EZH2:2.5 nM(Ki)
In vitro	METHODS: Synovial sarcoma cells Fuji and HS-SY-II were treated with Tazemetostat (0.039-20 µmol/L) for 14 days, and cell viability was measured using the CellTiter-Glo Luminescent Cell Viability Assay. RESULTS: Concentration-dependent reduction of cell proliferation was observed in Tazemetostat-treated Fuji and HS-SY-II cells, with IC50 values of 0.15 µmol/L and 0.52 µmol/L, respectively. [1] METHODS: Human renal cancer cells G401 and human malignant embryonic rhabdomyosarcoma cells RD were treated with Tazemetostat (0.006-1100 nM) for 4 days, and the expression levels of the target proteins were detected by Western Blot. RESULTS: Tazemetostat treatment resulted in a concentration-dependent decrease in overall H3K27Me3 levels. [2] Translated with DeepL.com (free version)
In vivo	METHODS: To assay antitumor activity in vivo, Tazemetostat (125-500 mg/kg, 0.5% NaCMC plus 0.1% Tween 80 in water) was administered orally to SCID mice harboring human renal carcinoma tumor G401 twice a day for twenty-eight days. RESULTS: Tazemetostat caused complete and sustained regression of SMARCB1 mutant MRT xenografts. [1] METHODS: To investigate the role in subarachnoid hemorrhage (SAH)-induced neuroinflammation, Tazemetostat (1-9 mg/kg) was administered intraperitoneally to a rat model of subarachnoid hemorrhage induced by endovascular perforation. RESULTS: Inhibition of EZH2 by Tazemetostat attenuated neuroinflammation after SAH in rats via the H3K27me3/SOCS3/TRAF6/NF-κB signaling pathway. [3]
Kinase Assay	Biochemical Methods: EPZ-6438 is incubated for 30 min with 40 μL per well of 5 nM PRC2 (final assay concentration in 50 μL is 4 nM ) in 1X assay buffer (20 mM Bicine [pH 7.6], 0.002% Tween-20, 0.005% Bovine Skin Gelatin and 0.5 mM DTT). 10 μL per well of substrate mix comprising assay buffer 3 H-SAM, unlabeled SAM, and peptide representing histone H3 residues 21-44 containing C-terminal biotin (appended to a C-terminal amide-capped lysine) are added to initiate the reaction (both substrates are present in the final reaction mixture at their respective Km values, an assay format referred to as ‘‘balanced conditions''. The final concentrations of substrates and methylation state of the substrate peptide are indicated for each enzyme Reactions are incubated for 90 min at room temperature and quenched with 10 μL per well of 600 μM unlabeled SAM, Then transferred to a 384-well flashplate and washed after 30 min.
Cell Research	For the adherent cell line proliferation assays, plating densities for each cell line are determined based on growth curves (measured by ATP content) and density over a 7-d time course. On the day before compound treatment, cells are plated in either 96-well plates in triplicate (for the day 0–7 time course) or 6-well plates (for replating on day 7 for the remainder of the time course). On day 0, cells are either untreated, DMSO-treated, or treated with EPZ-6438 starting at 10 μM and decreasing in either threefold or fourfold dilutions. Plates are read on day 0, day 4, and day 7 using Cell Titer Glo, with compound/media being replenished on day 4. On day 7, the six-well plates are trypsinized, centrifuged, and resuspended in fresh media for counting by Vi-Cell. Cells from each treatment are replated at the original density in 96-well plates in triplicate. Cells are allowed to adhere to the plate overnight, and cells are treated as on day 0. On days 7, 11, and 14, plates are read using Cell Titer Glo, with compound/media being replenished on day 11. Averages of triplicates are used to plot proliferation over the time course, and calculate IC50 values. For cell cycle and apoptosis, G401 and RD cells are plated in 15-cm dishes in duplicate at a density of 1 × 106 cells per plate. Cells are incubated with EPZ-6438 at 1 μM, in a total of 25 mL, over a course of 14 d, with cells being split back to original plating density on day 4, 7, and 11. Cell cycle analysis and TUNEL assay are performed using a Guava flow cytometer, following the manufacturer's protocol.(Only for Reference)

Synonyms	E-7438, EPZ6438
Molecular Weight	572.74
Formula	C34H44N4O4
CAS No.	1403254-99-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 33 mg/mL(57.6 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Kawano S, et al. Preclinical Evidence of Anti-Tumor Activity Induced by EZH2 Inhibition in Human Models of Synovial Sarcoma. PLoS One. 2016 Jul 8;11(7):e0158888. 2. Knutson SK, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZHProc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7. 3. Luo Y, et al. Inhibition of EZH2 (Enhancer of Zeste Homolog 2) Attenuates Neuroinflammation via H3k27me3/SOCS3/TRAF6/NF-κB (Trimethylation of Histone 3 Lysine 27/Suppressor of Cytokine Signaling 3/Tumor Necrosis Factor Receptor Family 6/Nuclear Factor-κB) in a Rat Model of Subarachnoid Hemorrhage. Stroke. 2020 Nov;51(11):3320-3331. 5. Cao Shangtao, Shengyong Yu, Dongwei Li, Jing Ye, Xuejie Yang, Chen Li, Xiaoshan Wang et al. Chromatin accessibility dynamics during chemical induction of pluripotency[J]. Cell stem cell. 2018 Apr 22(4): 529-542. e5.

Citations

1. Song P, Duan J L, Ding J, et al.Cellular senescence primes liver fibrosis regression through Notch‐EZH2.MedComm.2023, 4(5): e346. 2. Zhang Q, Chen X, Cao J, et al.Discovery of a Novel Covalent EZH2 Inhibitor Based on Tazemetostat Scaffold for the Treatment of Ovarian Cancer.Journal of Medicinal Chemistry.2023 3. Yang Y, Xiao L, Xue Y, et al.ZBTB7A regulates primed‐to‐naïve transition of pluripotent stem cells via recognition of the PNT‐associated sequence by Zinc Fingers 1–2 and recognition of γ‐globin− 200 gene element by Zinc Fingers 1–4.The FEBS Journal.2023 4. Gu T, Xu C, Meng X, et al.Sevoflurane Preconditioning Alleviates Posttraumatic Stress Disorder—Induced Apoptosis in the Hippocampus via the EZH2-Regulated Akt/mTOR Axis and Improves Synaptic Plasticity.Journal of Molecular Neuroscience.2023: 1-12. 5. Ghildiyal R, Sawant M, Renganathan A, et al. Loss of Long Noncoding RNA NXTAR in Prostate Cancer Augments Androgen Receptor Expression and Enzalutamide ResistanceTumor Suppressor lncRNA NXTAR Inhibits AR/AR-V7 Expression. Cancer Research. 2022, 82(1): 155-168 6. Ghildiyal R, Sawant M, Renganathan A, et al. Loss of long non-coding RNA NXTAR in prostate cancer augments androgen receptor expression and enzalutamide resistance. Cancer Research. 2021 7. Ghildiyal R, Sawant M, Renganathan A, et al. Loss of Long Noncoding RNA NXTAR in Prostate Cancer Augments Androgen Receptor Expression and Enzalutamide Resistance. Cancer Research. 2022, 82(1): 155-168 8. Luo Y, Fang Y, Kang R, et al. Inhibition of EZH2 (Enhancer of Zeste Homolog 2) Attenuates Neuroinflammation via H3k27me3/SOCS3/TRAF6/NF-κB (Trimethylation of Histone 3 Lysine 27/Suppressor of Cytokine Signaling 3/Tumor Necrosis Factor Receptor Family 6/Nuclear Factor-κB) in a Rat Model of Subarachnoid Hemorrhage. Stroke. 2020: STROKEAHA. 120.029951 9. Zhang L, Qu J, Qi Y, et al. EZH2 engages TGFβ signaling to promote breast cancer bone metastasis via integrin β1-FAK activation. Nature Communications. 2022, 13(1): 1-16 10. Cao Shangtao, Shengyong Yu, Dongwei Li, Jing Ye, Xuejie Yang, Chen Li, Xiaoshan Wang et al. Chromatin accessibility dynamics during chemical induction of pluripotency. Cell Stem Cell. 2018, 22(4): 529-542. e5

11. Yu S, Zhou C, Cao S, et al. BMP4 resets mouse epiblast stem cells to naive pluripotency through ZBTB7A/B-mediated chromatin remodelling. Nature cell biology. 2020: 1-12. 12. Yu S, Zhou C, He J, et al. BMP4 drives primed to naïve transition through PGC-like state. Nature Communications. 2022, 13(1): 1-15

See More... Hide

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Anti-Cancer Drug Library Highly Selective Inhibitor Library Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Target-Focused Phenotypic Screening Library Clinical Compound Library Drug-induced Liver Injury (DILI) Compound Library

Related Products

Related compounds with same targets

ZLD1039 SNDX-5613 Pinometostat JIB-04 Ryuvidine EEDi-5285 GNA002 BRD0639

Dose Conversion

You can also refer to dose conversion for different animals. More

In vivo Formulation Calculator (Clear solution)

Step One: Enter information below

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step Two: Enter the in vivo formulation

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

Calculate Reset

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Calculator

Molarity Calculator

Dilution Calculator

Reconstitution Calculation

Molecular Weight Calculator

Mass

Concentration

Volume

Molecular Weight

Molarity Calculator allows you to calculate the

Mass of a compound required to prepare a solution of known volume and concentration
Volume of solution required to dissolve a compound of known mass to a desired concentration
Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
Enter 10 into the Concentration box and select the correct unit (millimolar)
Enter 10 into the Volume box and select the correct unit (milliliter)
Press calculate
The answer of 19.713 mg appears in the Mass box

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

Calculator the dilution required to prepare a stock solution

Calculate the dilution required to prepare a stock solution
The dilution calculator is a useful tool which allows you to calculate how to dilute a stock solution of known concentration. Enter C1, C2 & V2 to calculate V1.

See Example

An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
Enter 10 into the Concentration (start) box and select the correct unit (millimolar)
Enter 50 into the Concentration (final) box and select the correct unit (micromolar)
Enter 20 into the Volume (final) box and select the correct unit (milliliter)
Press calculate
The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

Calculate the volume of solvent required to reconstitute your vial.

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial.
Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Molecule Formula

Molecular Weight g/mol

Enter the chemical formula of a compound to calculate its molar mass and elemental composition

Tip: Chemical formula is case sensitive: C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

bottom

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Tazemetostat 1403254-99-8 Chromatin/Epigenetic Histone Methyltransferase epigenetic inhibit EPZ-6438 Inhibitor E 7438 EPZ 6438 E7438 EZH1 cancer E-7438 EZH2 PRC2 EPZ6438 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.