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Tazemetostat (EPZ-6438)

Product Name
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
Formula Weight
572.74
MOL File
1403254-99-8.mol
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Tazemetostat (EPZ-6438) Property

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
pka
11.92±0.10(Predicted)
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.
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
16174
Product name
EPZ6438
Purity
≥98%
Packaging
1mg
Price
$44
Updated
2024/03/01
Cayman Chemical
Product number
16174
Product name
EPZ6438
Purity
≥98%
Packaging
5mg
Price
$130
Updated
2024/03/01
Cayman Chemical
Product number
16174
Product name
EPZ6438
Purity
≥98%
Packaging
10mg
Price
$235
Updated
2024/03/01
Cayman Chemical
Product number
16174
Product name
EPZ6438
Purity
≥98%
Packaging
50mg
Price
$745
Updated
2024/03/01
TRC
Product number
E592250
Product name
EPZ6438
Packaging
1mg
Price
$50
Updated
2021/12/16
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Tazemetostat (EPZ-6438) Chemical Properties,Usage,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

Preparation Products

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Tazemetostat (EPZ-6438) Suppliers

Shanghai Luofa Biochemical Technology Co., Ltd.
Tel
021-51111890 15317326293
Email
sales@molnova.com
Country
China
ProdList
4195
Advantage
58
Shanghai Jinsheng Pharmaceutical Co., Ltd.
Tel
1365-13651960330 13651960330
Email
xiangfeixia@jspharmatech.com
Country
China
ProdList
309
Advantage
58
Haisco Pharmaceutical Group Co., Ltd.
Tel
028-6725-0449 19382244693
Email
luoyan1@haisco.com
Country
China
ProdList
174
Advantage
58
Shanghai Hope Chem Co., Ltd.,
Tel
+21-18501659228 18501659228
Fax
sales@hope-chem.com
Email
info@hope-chem.com
Country
China
ProdList
483
Advantage
55
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
Adamas Reagent, Ltd.
Tel
400-6009262 16621234537
Fax
021-64823266
Email
chenyj@titansci.com
Country
China
ProdList
14103
Advantage
59
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
ProdList
4727
Advantage
58
NCE Biomedical Co.,Ltd.
Tel
4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988
Fax
+86-27-87599188
Country
China
ProdList
1493
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
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View Lastest Price from Tazemetostat (EPZ-6438) manufacturers

hebei hongtan Biotechnology Co., Ltd
Product
Tazemetostat (EPZ-6438) 1403254-99-8
Price
US $60.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
1000
Release date
2024-03-25
Hebei Weibang Biotechnology Co., Ltd
Product
Tazemetostat (EPZ-6438) 1403254-99-8
Price
US $5.90/kg
Min. Order
1kg
Purity
99%
Supply Ability
500000kg
Release date
2024-10-29
Hebei Mojin Biotechnology Co., Ltd
Product
Tazemetostat (EPZ-6438) 1403254-99-8
Price
US $0.00/KG
Min. Order
1KG
Purity
99%
Supply Ability
50000KG/month
Release date
2023-11-30

1403254-99-8, Tazemetostat (EPZ-6438) Related Search:


  • EPZ-6438
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  • [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
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  • EPZ6438;EPZ 6438;E-7438;TAZEMETOSTAT
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  • Tazemetostat (EPZ-6438) USP/EP/BP
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  • 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
  • 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
  • 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
  • 1403254-99-8
  • C34H44N4O4
  • Inhibitors