Product Name

Tazemetostat (EPZ-6438)

General description

Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor.

Purity

≥98.0%(HPLC)

CAS Number

1403254-99-8

Formula

C³⁴H⁴⁴N⁴O⁴

Molecular Weight

572.74

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

solid

Solubility(25℃)

DMSO

~5mg/mL(warmed)

Ethanol

Insoluble

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Tazemetostat is an orally available, small molecule selective and S-adenosyl methionine (SAM) competitive inhibitor of histone methyl transferase EZH2, with potential antineoplastic activity. Upon oral administration, tazemetostat selectively inhibits the activity of both wild-type and mutated forms of EZH2. Inhibition of EZH2 specifically prevents the methylation of histone H3 lysine 27 (H3K27). This decrease in histone methylation alters gene patterns associated with cancer pathways and results in decreased tumor cell proliferation in EZH2 mutated cancer cells. EZH2, which belongs to the class of histone methyltransferases (HMTs), is overexpressed or mutated in a variety of cancer cells and plays a key role in tumor cell proliferation.

Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with Ki and IC50 of 2.5 nM and 11 nM in cell-free assays, exhibiting a 35-fold selectivity versus EZH1 and >4,500-fold selectivity relative to 14 other HMTs.

Application

Tazemetostat has been used in trials studying the treatment of Rhabdoid Tumors, Synovial Sarcoma, Epithelioid sarcoma, INI1-negative Tumors, and Renal Medullary Carcinoma, among others.

l  Storage

Storage temp.

-20℃

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov