1. Epigenetics
  2. Histone Methyltransferase
  3. Tazemetostat hydrobromide

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

Cat. No.: HY-13803C Purity: 99.18%
Handling Instructions

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

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

Tazemetostat hydrobromide Chemical Structure

Tazemetostat hydrobromide Chemical Structure

CAS No. : 1467052-75-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 503 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1650 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Tazemetostat hydrobromide:

Top Publications Citing Use of Products

    Tazemetostat hydrobromide 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 hydrobromide 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 hydrobromide 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

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    • References

    • Customer Review

    Description

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

    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

    653.65

    Formula

    C₃₄H₄₅BrN₄O₄

    CAS No.

    1467052-75-0

    SMILES

    O=C(C1=CC(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(CC)C4CCOCC4)=C1C)NCC5=C(C)C=C(C)NC5=O.[H]Br

    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 : 100 mg/mL (152.99 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5299 mL 7.6494 mL 15.2987 mL
    5 mM 0.3060 mL 1.5299 mL 3.0597 mL
    10 mM 0.1530 mL 0.7649 mL 1.5299 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: ≥ 2.5 mg/mL (3.82 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (3.82 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (3.82 mM); Clear solution

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

    Purity: 99.18%

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    Product name:
    Tazemetostat hydrobromide
    Cat. No.:
    HY-13803C
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