Tazemetostat hydrobromide

SKU: orb1940692

Description

Tazemetostat hydrobromide is a potent and selective EZH2 inhibitor. Tazemetostat hydrobromide inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 (Ki: 2.5 nM). Tazemetostat hydrobromide also inhibits EZH1 (IC50: 392 nM).(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 .(In Vivo):Tazemetostat (250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors .

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1467052-75-0
• MW: 653.662
• Purity: >98% (HPLC)
• Formula: C₃₄H₄₅BrN₄O₄
• SMILES: Br.CCN(C1CCOCC1)c1cc(cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)-c1ccc(CN2CCOCC2)cc1
• Target: Histone Demethylase

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EPZ-6438 hydrobromide | E-7438 hydrobromide

Quick Database Links

Gene Symbol

Histone Demethylase