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Tazemetostat (EPZ-6438)

Tazemetostat (EPZ-6438) Suppliers list
Tel: +undefined-21-51877795
Products Intro: Product Name:EPZ6438
Purity:98% Package:10MG;50MG;100MG,1G,5G,10G.100G
Company Name: Hebei Mojin Biotechnology Co., Ltd
Tel: +8613288715578
Products Intro: Product Name:Tazemetostat (EPZ-6438)
Purity:99% Package:25KG
Company Name: hebei hongtan Biotechnology Co., Ltd
Tel: +86-86-1913198-3935 +8617331935328
Products Intro: Product Name:Tazemetostat (EPZ-6438)
Purity:99% Package:1kg;60USD
Company Name: career henan chemical co
Tel: +86-0371-86658258
Products Intro: Product Name:EPZ-6438
Purity:98-100% Package:1KG;1USD
Company Name: TianYuan Pharmaceutical CO.,LTD
Tel: +86-755-23284190 13684996853
Products Intro: Product Name:EPZ6438
Purity:99% Package:10g 100g 200g 500g 1kg 5kg per barrel

Tazemetostat (EPZ-6438) manufacturers

  • Tazemetostat (EPZ-6438)
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  • $0.00 / 25KG
  • 2023-11-30
  • CAS:1403254-99-8
  • Min. Order: 1KG
  • Purity: 99%
  • Supply Ability: 50000KG/month
Tazemetostat (EPZ-6438) Basic information
Product Name:Tazemetostat (EPZ-6438)
Synonyms: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)
Product Categories:Inhibitors
Mol File:1403254-99-8.mol
Tazemetostat (EPZ-6438) Structure
Tazemetostat (EPZ-6438) Chemical 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).
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.
Safety Information
MSDS Information
Tazemetostat (EPZ-6438) Usage And Synthesis
DescriptionTazemetostat (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
UsesEPZ 6438 is a potent and selective inhibitor of EZH2.
Biological ActivityTazemetostat (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.
targetEZH2(Cell-free assay)
References1) 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
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