EPZ6438

Data Sheet For research use only. Not for human use.

Cat. No. ：BCP07409CAS No. ：1403254-99-8Purity：98%

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CAS No.	1403254-99-8	Cat. No.	BCP07409
Name	EPZ6438
Synonyms	EPZ-6438; EPZ 6438; E7438; Tazemetostat; E-7438; E 7438;
SMILES	CCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCOCC5
Chemical Name
Formula	C34H44N4O4	M. Wt	572.74
Purity	98%	Storage	Store at 4-8°C
Description	Tazemetostat, also known as EPZ-6438 and E7438, is a potent, selective, and orally bioavailable small-molecule inhibitor of EZH2 enzymatic activity. EPZ-6438 induces apoptosis and differentiation specifically in SMARCB1-deleted MRT cells. Treatment of xenograft-bearing mice with EPZ-6438 leads to dose-dependent regression of MRTs with correlative diminution of intratumoral trimethylation levels of lysine 27 on histone H3, and prevention of tumor regrowth after dosing cessation. These data demonstrate the dependency of SMARCB1 mutant MRTs on EZH2 enzymatic activity and portend the utility of EZH2-targeted drugs for the treatment of these genetically defined cancers.EPZ-6438 is currently in clinical trials.