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EPZ-6438 - CAS 1403254-99-8

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Catalog Number	Size	Price	Stock	Quantity
BP-300154	1 g	$519	In stock

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EPZ-6438 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.

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Molecular Formula

C34H44N4O4

Molecular Weight

572.75

EPZ-6438

- Specification
  - Purity
    
    98%
    
    Appearance
    
    White to off-white powder
    
    Storage
    
    2 - 8 °C
    
    IUPAC Name
    
    N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide
    
    Synonyms
    
    EPZ-6438; EPZ 6438; EPZ6438; E7438; E-7438; E 7438; Tazemetostat
- Properties
  - InChI Key
    
    NSQSAUGJQHDYNO-UHFFFAOYSA-N
    
    InChI
    
    InChI=1S/C34H44N4O4/c1-5-38(29-10-14-41-15-11-29)32-20-28(27-8-6-26(7-9-27)22-37-12-16-42-17-13-37)19-30(25(32)4)33(39)35-21-31-23(2)18-24(3)36-34(31)40/h6-9,18-20,29H,5,10-17,21-22H2,1-4H3,(H,35,39)(H,36,40)
    
    Canonical SMILES
    
    CCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCOCC5
- Reference Reading
  - 1.Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma.
    
    Knutson SK1, Kawano S, Minoshima Y, Warholic NM, Huang KC, Xiao Y, Kadowaki T, Uesugi M, Kuznetsov G, Kumar N, Wigle TJ, Klaus CR, Allain CJ, Raimondi A, Waters NJ, Smith JJ, Porter-Scott M, Chesworth R, Moyer MP, Copeland RA, Richon VM, Uenaka T, Pollock Mol Cancer Ther. 2014 Apr;13(4):842-54. doi: 10.1158/1535-7163.MCT-13-0773. Epub 2014 Feb 21.
    
    Mutations within the catalytic domain of the histone methyltransferase EZH2 have been identified in subsets of patients with non-Hodgkin lymphoma (NHL). These genetic alterations are hypothesized to confer an oncogenic dependency on EZH2 enzymatic activity in these cancers. We have previously reported the discovery of EPZ005678 and EPZ-6438, potent and selective S-adenosyl-methionine-competitive small molecule inhibitors of EZH2. Although both compounds are similar with respect to their mechanism of action and selectivity, EPZ-6438 possesses superior potency and drug-like properties, including good oral bioavailability in animals. Here, we characterize the activity of EPZ-6438 in preclinical models of NHL. EPZ-6438 selectively inhibits intracellular lysine 27 of histone H3 (H3K27) methylation in a concentration- and time-dependent manner in both EZH2 wild-type and mutant lymphoma cells. Inhibition of H3K27 trimethylation (H3K27Me3) leads to selective cell killing of human lymphoma cell lines bearing EZH2 catalytic domain point mutations.
- Preparing Stock Solutions
  - ConcentrationVolumeMass 1 mg 5 mg 10 mg
    
    1 mM 1.7460 mL 8.7300 mL 17.4599 mL
    
    5 mM 0.3492 mL 1.7460 mL 3.4920 mL
    
    10 mM - - -
    
    50 mM - - -

ConcentrationVolumeMass	1 mg	5 mg	10 mg
1 mM	1.7460 mL	8.7300 mL	17.4599 mL
5 mM	0.3492 mL	1.7460 mL	3.4920 mL
10 mM	-	-	-
50 mM	-	-	-

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