Tazemetostat (EPZ-6438)

Catalog No.S7128 Synonyms: E7438

Tazemetostat (EPZ-6438) Chemical Structure

Molecular Weight(MW): 572.74

Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.

Size Price Stock Quantity  
USD 197 In stock
USD 670 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

2 Customer Reviews

  • we examined the E-cadherin, ZEB1 and Snail expressions after using EZH2 RNAi, DZNeP and EPZ-6438. “*”represent P<0.05 when compared with control group.

    Oncotarget, 2016, 7(10):11194-207. Tazemetostat (EPZ-6438) purchased from Selleck.

    EZH2 inhibition does not affect pediatric high-grade glioma cell growth in vitro. (a-c) Relative cell viability of pediatric high-grade glioma cell lines were subjected to MTT cell viability assays 72 h after incubation with increasing concentrations of Tazemetostat (EPZ-6438) as indicated. Graphs show the mean of 3 independent biological replicates with the respective SEM, * p < 0.05.

    Klin Padiatr, 2016, 228(3):113-117.. Tazemetostat (EPZ-6438) purchased from Selleck.

Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.
Features Orally bioavailable EZH2-selective inhibitor for both wild-type and mutant. Currently being tested in Phase II clinical trials for treatment of Diffuse Large B Cell Lymphoma.
Targets
EZH2 [1]
(Cell-free assay)
EZH2 [1]
(Cell-free assay)
2.5 nM(Ki) 2.5 nM(Ki)
In vitro

EPZ-6438 concentration-dependently reduces global H3K27Me3 levels in wild-type or SMARCB1 mutant cells, and induces strong antiproliferative effects with IC50 ranging from 32 nM to 1000 nM in SMARCB1-deleted MRT cell lines. EPZ-6438 induces gene expression of neuronal differentiation and cell cycle inhibition, while inhibtis expression of Hedgehog pathway genes, MYC and EZH2. [1] The antiproliferative effect of EPZ-6438 is enhanced by either prednisolone or dexamethasone in several EZH2 mutant lymphoma cell lines. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells MYPGeY5kfGmxbjDhd5NigQ>? NITDdmU4OiCq NGrXUlNKdmirYnn0bY9vKG:oIFXaTFIhcW5iaIXtZY4hUGWOYTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gbY4hUDONMkft[VMhdGW4ZXzzJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IFXMTXNCKG2ndHjv[EwhUUN3ME2wMlAzKM7:TT6= NYLmSFhyOjZzOEmwO|g>

... Click to View More Cell Line Experimental Data

In vivo In SCID mice bearing s.c. G401 xenografts, EPZ-6438 induces tumor stasis during the administration period and produces a significant tumor growth delay with minimal effect on body weight. [1]

Protocol

Kinase Assay:[1]
+ Expand

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:[1]
+ Expand
  • Cell lines: Mutant cell lines (G401, A204, G402, KYM-1), Wild type cell line (RD, 293, SJCRH30)
  • Concentrations: ~10 μM
  • Incubation Time: 7 days
  • Method: 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)
Animal Research:[1]
+ Expand
  • Animal Models: SCID mice bearing s.c. G401 xenografts.
  • Formulation: 0.5% NaCMC plus 0.1% Tween 80 in water
  • Dosages: ~500 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL warmed (8.72 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 2.5mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 572.74
Formula

C34H44N4O4

CAS No. 1403254-99-8
Storage powder
in solvent
Synonyms E7438

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

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

Total Molecular Weight: g/mol

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 in 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01897571 Recruiting B-cell Lymphomas (Phase 1)|Advanced Solid Tumors (Phase 1)|Diffuse Large B-cell Lymphoma (Phase 2)|Follicular Lymphoma (Phase 2)|Transformed Follicular Lymphoma|Primary Mediastinal Large B-Cell Lymphoma Epizyme, Inc. June 2013 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Histone Methyltransferase Signaling Pathway Map

Tags: buy Tazemetostat (EPZ-6438) | Tazemetostat (EPZ-6438) supplier | purchase Tazemetostat (EPZ-6438) | Tazemetostat (EPZ-6438) cost | Tazemetostat (EPZ-6438) manufacturer | order Tazemetostat (EPZ-6438) | Tazemetostat (EPZ-6438) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID