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Tazemetostat (EPZ-6438)

Tazemetostat (EPZ-6438) structure

CAS No.: 1403254-99-8

Chemical Name:: Tazemetostat (EPZ-6438)

Synonyms: Tazemetostat;EPZ-6438;E-7438;CS-971;CPDB1064;EPZ-7438;EPZ-6438(E7438);E7438, Tazemetostat;Tazemetostat EPZ-6438;Henagliflozin Proline

CBNumber:: CB82655404

Molecular Formula:: C34H44N4O4

Molecular Weight:: 572.74

MDL Number:: MFCD24849415

MOL File:: 1403254-99-8.mol

Last updated:2024-03-25 11:48:53

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Tazemetostat (EPZ-6438) Properties

Melting point	>162°C (dec.)
Boiling point	750.8±60.0 °C(Predicted)
Density	1.163±0.06 g/cm3(Predicted)
storage temp.	-20°C
solubility	Soluble in DMSO (up to at least 25 mg/ml).
pka	11.92±0.10(Predicted)
form	solid
color	Off-white
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
FDA UNII	Q40W93WPE1

SAFETY

Risk and Safety Statements

Symbol(GHS)

GHS07

Signal word

Warning

Hazard statements

H302-H315-H319-H335

Precautionary statements

P261-P264-P270-P271-P280-P301+P312-P330-P302+P352-P321-P304+P340-P305+P351+P338-P332+P313-P362+P364-P337+P313-P403+P233-P405-P501

NFPA 704

	0
2		0

Tazemetostat (EPZ-6438) price More Price(37)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
Cayman Chemical	16174	EPZ6438 ≥98%	1403254-99-8	1mg	$44	2024-03-01	Buy
Cayman Chemical	16174	EPZ6438 ≥98%	1403254-99-8	5mg	$130	2024-03-01	Buy
Cayman Chemical	16174	EPZ6438 ≥98%	1403254-99-8	10mg	$235	2024-03-01	Buy
Cayman Chemical	16174	EPZ6438 ≥98%	1403254-99-8	50mg	$745	2024-03-01	Buy
TRC	E592250	EPZ6438	1403254-99-8	1mg	$50	2021-12-16	Buy

Product number	Packaging	Price	Buy
16174	1mg	$44	Buy
16174	5mg	$130	Buy
16174	10mg	$235	Buy
16174	50mg	$745	Buy
E592250	1mg	$50	Buy

Tazemetostat (EPZ-6438) Chemical Properties,Uses,Production

Description

Tazemetostat (1403254-99-8) is a potent (Ki = 2.5nM wild type human PRC2-containing) and selective SAM-competitive inhibitor of the lysine methyltransferase EZH2.1?Tazemetostat displayed strong antiproliferative effects against SMARCB1-deleted malignant rhabdoid tumor (MRT) cell lines?in vitro. This antitumor activity was also observed in SMARTCB1 mutant mouse xenografts. It displayed potent antitumor activity in various cancer models including non-Hodgkins lymphoma2, pediatric glioma3, small-cell carcinoma of the ovary4, and synovial sarcomas5. 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.6

Uses

EPZ 6438 is a potent and selective inhibitor of EZH2.

Biological Activity

Tazemetostat (EPZ-6438) is a potent, and selective EZH2 inhibitor with K i 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 HMT.

target

EZH2(Cell-free assay)

References

1) Knutson?et al.?(2013),?Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2;?Proc. Natl. Acad. Sci. USA?110?7922 2) Knutson?et al.?(2014),?Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma; Mol.Cancer Ther.?13?842 3) Mohammad?et al. (2017),?EZH2 is a potential therapeutic target for H3K27M-mutant pediatric gliomas; Nat. Med.?23?483 4) Chan-Penebre?et al.?(2017),?Selective killing of SMARCA2- and SMARCA4-deficient Small Cell Carcinoma of the Ovary, Hypercalcemic Type Cells by Inhibition of EZH2: In Vitro and In Vivo Preclinical Models; Mol. Cancer Ther.?16?850 5) Kawano?et al.?(2016),?Preclinical Evidence of Anti-Tumor Activity by EZH2 Inhibition in Human Models of Synovial Sarcoma; PLoS One?11?e0158888 6) Arifuzzaman?et al.?(2017),?Selective inhibition of EZH2 by a small molecule inhibitor regulates microglial gene expression essential for inflammation; Biochem. Pharmacol.?137?61

Tazemetostat (EPZ-6438) synthesis

Synthesis of Tazemetostat (EPZ-6438) from 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- and 4-[4-(4,4,5,5-TETRAMETHYL-1,3,2-DIOXABOROLAN-2-YL)BENZYL]MORPHOLINE

Tazemetostat (EPZ-6438) Preparation Products And Raw materials

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-

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Preparation Products

Tazemetostat (EPZ-6438) Suppliers

Global( 191)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
Hebei Mojin Biotechnology Co., Ltd	+8613288715578	sales@hbmojin.com	China	12453	58
hebei hongtan Biotechnology Co., Ltd	+86-86-1913198-3935 +8617331935328	sales03@chemcn.cn	China	951	58
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
TianYuan Pharmaceutical CO.,LTD	+86-755-23284190 13684996853	sales@tianpharm.com	CHINA	304	58
Hainan Xiyuan Chemical Technology Co., Ltd.	+86-15008981366	15008981366@163.com	CHINA	9	58
Biochempartner	0086-13720134139	candy@biochempartner.com	CHINA	967	58
Hubei Jusheng Technology Co.,Ltd.	18871490254	linda@hubeijusheng.com	CHINA	28180	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58

Supplier	Advantage
ATK CHEMICAL COMPANY LIMITED	60
Hebei Mojin Biotechnology Co., Ltd	58
hebei hongtan Biotechnology Co., Ltd	58
career henan chemical co	58
TianYuan Pharmaceutical CO.,LTD	58
Hainan Xiyuan Chemical Technology Co., Ltd.	58
Biochempartner	58
Hubei Jusheng Technology Co.,Ltd.	58
BOC Sciences	58
Chongqing Chemdad Co., Ltd	58

View Lastest Price from Tazemetostat (EPZ-6438) manufacturers

Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
2024-04-12	Tazemetostat (EPZ-6438) 1403254-99-8	US $60.00 / kg	1kg	99%	1000	hebei hongtan Biotechnology Co., Ltd
2023-11-30	Tazemetostat (EPZ-6438) 1403254-99-8	US $0.00 / KG	1KG	99%	50000KG/month	Hebei Mojin Biotechnology Co., Ltd
2023-09-06	Tazemetostat (EPZ-6438) 1403254-99-8	US $0.00-0.00 / KG	1KG	99%	500000kg	Hebei Guanlang Biotechnology Co., Ltd.

Tazemetostat (EPZ-6438)
1403254-99-8
US $60.00 / kg
99%
hebei hongtan Biotechnology Co., Ltd

Tazemetostat (EPZ-6438)
1403254-99-8
US $0.00 / KG
99%
Hebei Mojin Biotechnology Co., Ltd

Tazemetostat (EPZ-6438)
1403254-99-8
US $0.00-0.00 / KG
99%
Hebei Guanlang Biotechnology Co., Ltd.

Tazemetostat (EPZ-6438) Spectrum

Tazemetostat (EPZ-6438)(1403254-99-8)MS

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E-7438 EPZ-7438 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 [1,1'-Biphenyl]-3-carboxamide, 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)- 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 EPZ6438 Henagliflozin Proline Tazemetostat EPZ-6438 EPZ-6438(E7438) N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino CPDB1064 EPZ6438(Tazemetostat) 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 E7438, Tazemetostat N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)biphenyl-3-carboxamide EPZ6438;EPZ 6438;E-7438;TAZEMETOSTAT CS-971 E7438,EPZ6438, EPZ-6438 EPZ6438; EPZ 6438; E-7438 [1,1'-Biphenyl]-3-carboxamide Tazemetostat (EPZ-6438) USP/EP/BP N-[(4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-5-[ethyl(tetrahydropyran-4-yl)amino]-4-methyl-4'-(morpholinomethyl)biphenyl-3-carboxamide EPZ-6438 Tazemetostat N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide EPZ6438 Tazemetostat EPZ-6438 EPZ 6438,epigenetic,inhibit,E 7438,Tazemetostat,Histone Methyltransferase,EPZ-6438,Inhibitor,E7438,EZH1,cancer,EZH2,PRC2 1403254-99-8 C34H44N4O4 Inhibitors