1. Epigenetics
  2. Histone Methyltransferase
  3. Tazemetostat

Tazemetostat (Synonyms: EPZ-6438; E-7438)

Cat. No.: HY-13803 Purity: 99.76%
Handling Instructions

Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.

For research use only. We do not sell to patients.

Tazemetostat Chemical Structure

Tazemetostat Chemical Structure

CAS No. : 1403254-99-8

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 76 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 84 In-stock
Estimated Time of Arrival: December 31
50 mg USD 120 In-stock
Estimated Time of Arrival: December 31
100 mg USD 190 In-stock
Estimated Time of Arrival: December 31
200 mg USD 290 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Tazemetostat:

Top Publications Citing Use of Products

    Tazemetostat purchased from MCE. Usage Cited in: Toxins (Basel). 2017 May 16;9(5). pii: E162.

    Cells are treated with LeTx in the presence or absence of GSK-J4 or EPZ-6438 for 48 h. H3K27me3 level is analyzed by Western blotting.

    Tazemetostat purchased from MCE. Usage Cited in: J Clin Invest. 2018 Jan 2;128(1):483-499.

    Immunoblotting for N1-ICD (n=3) in mouse podocytes exposed to 10 μM EPZ-6438 for 48 hours.

    Tazemetostat purchased from MCE. Usage Cited in: Nat Struct Mol Biol. 2018 Mar;25(3):225-232.

    Western blots of extracts from E14 mESCs treated with 10 μM. EPZ6438 EZH2 inhibitor for 7 d and sampled at time points following inhibitor washout. Blots are probed with the indicated antibodies.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM[1].

    IC50 & Target[1]

    EZH2 WT

    2.5 nM (Ki)

    EZH2

    11 nM (IC50, in peptide assay)

    EZH2

    16 nM (IC50, in nucleosome assay)

    Rat EZH2

    4 nM (IC50)

    EZH1

    392 nM (IC50)

    In Vitro

    Tazemetostat (EPZ-6438) inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM[1].

    Cell Proliferation Assay[1]

    Cell Line: Wild-type and mutant lymphoma cell lines: DOHH-2 cell (EZH2 wild-type), Farage cell (EZH2 wild-type), OCI-LY19 cell (EZH2 wild-type), Toledo cell (EZH2 wild-type), KARPAS-422 (EZH2 Y646N), Pfeiffer (EZH2 A682G), RL cell line (EZH2 Y646N), SU-DHL-10 (EZH2 Y646F), SU-DHL-6 (EZH2 Y646N), WSU-DLCL2 (EZH2 Y646F)
    Concentration: 0.49 nM-7.6 μM
    Incubation Time: 11 days
    Result: Inhibited DOHH-2 cell (EZH2 wild-type; IC50=1.7 μM), Farage cell (EZH2 wild-type; IC50=99 nM), OCI-LY19 cell (EZH2 wild-type; IC50=6.2 μM), Toledo cell (EZH2 wild-type; IC50=7.6 μM), KARPAS-422 (EZH2 Y646N; IC50=1.8 nM), Pfeiffer (EZH2 A682G; IC50=0.49 nM), RL cell line (EZH2 Y646N; IC50=5.8 μM), SU-DHL-10 (EZH2 Y646F; IC50=5.8 nM), SU-DHL-6 (EZH2 Y646N; IC50=4.7 nM), WSU-DLCL2 (EZH2 Y646F; IC50=8.6 nM) proliferation.
    In Vivo

    Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors[1].

    Animal Model: SCID mice bearing s.c. G401 xenografts [1]
    Dosage: 125 mg/kg, 250 mg/kg, 500 mg/kg
    Administration: Oral; twice daily ; 28 days
    Result: Practically eliminated the fast-growing G401 tumors at 250 or 500 mg/kg.
    Molecular Weight

    572.74

    Formula

    C₃₄H₄₄N₄O₄

    CAS No.

    1403254-99-8

    SMILES

    O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(CC)C4CCOCC4)=C1C)NCC5=C(C)C=C(C)NC5=O

    Shipping

    Room temperature in continental US; may vary elsewhere

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 33 mg/mL (57.62 mM; Need ultrasonic)

    0.1 M HCL : 14.29 mg/mL (24.95 mM; ultrasonic and adjust pH to 5 with HCl)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7460 mL 8.7300 mL 17.4599 mL
    5 mM 0.3492 mL 1.7460 mL 3.4920 mL
    10 mM 0.1746 mL 0.8730 mL 1.7460 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.76%

    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Tazemetostat
    Cat. No.:
    HY-13803
    Quantity: