Tazemetostat hydrobromide

SKU: orb1307697

Description

Tazemetostat hydrobromide is a potent, selective inhibitor of EZH2 (Ki=2.5 nM) and EZH1 (IC50=392 nM), targeting the PRC2 complex. It is widely used in oncology research to study epigenetic mechanisms in vitro and has demonstrated antitumor efficacy in various preclinical in vivo models.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1467052-75-0
• MW: 653.65
• Purity: 99.80% (May vary between batches)
• Formula: C₃₄H₄₅BrN₄O₄
• 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
• Target: Histone Methyltransferase
• Solubility: DMSO:102 mg/mL (156.05 mM)

Bioactivity

• Target IC50:
  EZH2 (WT):2.5 nM (Ki)|EZH2:11 nM (in peptide assay)|EZH2:16 nM (in nucleosome assay)|EZH2 (rat):4 nM|EZH1:392 nM
• In Vivo:
  Tazemetostat (250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors .
• In Vitro:
  Tazemetostat hydrobromide inhibits Rat EZH2 (IC50: 4 nM). Tazemetostat hydrobromide inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat hydrobromide inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC50s of 0.49 nM-7.6 μM .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tazemetostat, Tazemetostat Hydrobromide, Tazemetostat hydrobromide, Rat EZH2, PRC2, cancer, E 7438, E 7438 Hydrobromide, E-7438, E7438, E7438 Hydrobromide, E-7438 hydrobromide, E-7438 Hydrobromide, inhibit, HistoneMethyltransferase, Histone Methyltransferase, Inhibitor, EZH2, EZH2 WT, EZH1, epigenetic, EPZ 6438, EPZ 6438 Hydrobromide, EPZ6438, EPZ-6438, EPZ6438 Hydrobromide, EPZ-6438 Hydrobromide, EPZ-6438 hydrobromide

Compound Identifiers

PubChem CID

71761627