Name: EPZ-6438
Brand: BOC Sciences
Price: 519 USD
Availability: MadeToOrder

Size

Price

Stock

Quantity

1 g

$519

In stock

Purity

98%

Appearance

White to off-white powder

Storage

2 - 8 °C

IUPACName

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

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

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.

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	-	-	-

HNMR

HPLC

I want to know what are the synthetic materials of EPZ-6438?

Raw materials：BenzaMide, 5-broMo-N-[(1,2-dihydro-4,6-diMethyl-2-oxo-3-pyridinyl)Methyl]-3-[ethyl(tetrahydro-2H-pyran-4-yl)aMino]-2-Methyl--->Benzoic acid, 5-broMo-2-Methyl-3-[(tetrahydro-2H-pyran-4-yl)aMino]-, Methyl ester-->3-(aMinoMethyl)-4,6-diMethyl-1,2-dihydropyridin-2-one hydrochloride-->Methyl 3-AMino-5-broMo-2-Methylbenzoate-->5-BROMO-2-METHYL-3-NITROPHENYL METHYLCARBOXYLATE-->4-[4-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)BENZYL]MORPHOLINE-->Benzoic acid, 5-broMo-3-[ethyl(tetrahydro-2H-pyran-4-yl)aMino]-2-Methyl-, Methyl ester-->5-BROMO-2-METHYL-3-NITROBENZOIC ACID-->Benzoic acid, 5-broMo-3-[ethyl(tetrahydro-2H-pyran-4-yl)aMino]-2-Methyl-

13/7/2019

Hello, is EPZ-6438 selective?

EPZ-6438 is an effective selective EZH2 inhibitor, with K i and IC50 of 2.5 nM and 11 nM, respectively.

13/4/2022

I would like to know if EPZ-6438 can induce cell apoptosis?

EPZ-6438 specifically induces cell apoptosis and differentiation in SMARCB1 deficient MRT cells.

23/7/2023

has a 35 fold higher selectivity for inhibiting EZH2

We are very satisfied with EPZ-6438. Compared with EZH1, it has a 35 fold higher selectivity for inhibiting EZH2, and more than 4500 times higher selectivity compared to the other 14 HMTs.

23/10/2017

resulted in a related decrease in tumor induced trimethylation levels of lysine 27 on histone H3

In our mouse experiment, the use of EPZ-6438 resulted in a related decrease in tumor induced trimethylation levels of lysine 27 on histone H3.

31/10/2018

resulted in dose-dependent regression of MRTs

In our study, the treatment of mice carrying xenografts with EPZ-6438 resulted in dose-dependent regression of MRTs.

12/8/2019

Stock concentration: *

Desired final volume: *

Desired concentration: *

* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C₁V₁ = C₂V₂