Tazemetostat (EPZ-6438)
- 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
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 |
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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 |
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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 |
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) Preparation Products And Raw materials
Raw materials
1of2
Preparation Products
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
Hebei Mujin Biotechnology Co.,Ltd | +86 13288715578 +8613288715578 | sales@hbmojin.com | China | 12826 | 58 |
Hebei Weibang Biotechnology Co., Ltd | +8617732866630 | bess@weibangbio.com | China | 18147 | 58 |
hebei hongtan Biotechnology Co., Ltd | +86-86-1913198-3935 +8617331935328 | sales03@chemcn.cn | China | 970 | 58 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32965 | 60 |
career henan chemical co | +86-0371-86658258 +8613203830695 | sales@coreychem.com | China | 29871 | 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 | 965 | 58 |
Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28172 | 58 |
Accela ChemBio Inc. | +1-858-6993322 | info@accelachem.com | United States | 18478 | 58 |
View Lastest Price from Tazemetostat (EPZ-6438) manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
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2025-02-18 | Tazemetostat (EPZ-6438)
1403254-99-8
|
US $0.00 / KG | 1KG | 99% | 50000KG/month | Hebei Mujin Biotechnology Co.,Ltd | |
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2025-02-17 | Tazemetostat (EPZ-6438)
1403254-99-8
|
US $60.00 / kg | 1kg | 99% | 1000 | hebei hongtan Biotechnology Co., Ltd | |
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2024-11-19 | Tazemetostat
1403254-99-8
|
US $59.00-113.00 / mg | ≥95% | 10g | TargetMol Chemicals Inc. |
-
- Tazemetostat (EPZ-6438)
1403254-99-8
- US $0.00 / KG
- 99%
- Hebei Mujin Biotechnology Co.,Ltd
-
- Tazemetostat (EPZ-6438)
1403254-99-8
- US $60.00 / kg
- 99%
- hebei hongtan Biotechnology Co., Ltd
-
- Tazemetostat
1403254-99-8
- US $59.00-113.00 / mg
- ≥95%
- TargetMol Chemicals Inc.