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

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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:

GDC-0032 tasquinimod GDC-0084 SH-4-54 Osimertinib mesylate Niraparib Mertansine (S)-tert-butyl 2-(4-(4-chlorophenyl)-2,3,9-triMethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetate Enasidenib Ivosidenib ABBV-075 Ponatinib Selonsertib Panobinostat GSK 343 (2R,3R,4S,5R)-2-(6-aMino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]iMidazol-2-yl)ethyl)cyclobutyl)(isopropyl)aMino)Methyl)tetrahydrofuran-3,4-diol MM-102 UNC 1999

EPZ-6438

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

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

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

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

1403254-99-8

C34H44N4O4

Inhibitors