Tazemetostat, EZH2 inhibitor (TBI4032)

Description

Product Details

Formal Name: N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-5-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-4-methyl-4′-(4-morpholinylmethyl)-[1,1′-biphenyl]-3-carboxamide

Alternate Names: EPZ-6438

Molecular Formula: C₃₄H₄₄N₄O₄

Formula Weight: 572.80

CAS Number: 1403254-99-8

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

EZH2 inhibitor

Functions

Potent and selective SAM-competitive inhibitor of the lysine methyltransferase EZH2 (Ki = 2.5nM wild type human PRC2-containing). Displayed strong antiproliferative effects against SMARCB1-deleted malignant rhabdoid tumor (MRT) cell lines in vitro. Antitumor activity was also observed in SMARTCB1 mutant mouse xenografts. Displays potent antitumor activity in various cancer models including non-Hodgkins lymphoma, pediatric glioma, small-cell carcinoma of the ovary, and synovial sarcomas. Tazemetostat has also been shown to control inflammatory genes by modulating IRF1, IRF8, and STAT1 levels suggesting therapeutic potential for the treatment of neuroinflammatory diseases associated with microglial activation.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 1 month.