1403257-79-3

Basic information

• Product Name: Benzoic acid, 5-broMo-3-[ethyl(tetrahydro-2H-pyran-4-yl)aMino]-2-Methyl-, Methyl ester
• Synonyms: Benzoic acid, 5-broMo-3-[ethyl(tetrahydro-2H-pyran-4-yl)aMino]-2-Methyl-, Methyl ester;methyl 5-bromo-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-methylbenzoate
• CAS NO: 1403257-79-3
• Molecular Formula: C₁₆H₂₂BrNO₃
• Molecular Weight: 356.25478
• Mol File: 1403257-79-3.mol
• Article Data: 27

Chemical Properties

• Appearance: /
• CAS DataBase Reference: Benzoic acid, 5-broMo-3-[ethyl(tetrahydro-2H-pyran-4-yl)aMino]-2-Methyl-, Methyl ester(CAS DataBase Reference)
• NIST Chemistry Reference: Benzoic acid, 5-broMo-3-[ethyl(tetrahydro-2H-pyran-4-yl)aMino]-2-Methyl-, Methyl ester(1403257-79-3)
• EPA Substance Registry System: Benzoic acid, 5-broMo-3-[ethyl(tetrahydro-2H-pyran-4-yl)aMino]-2-Methyl-, Methyl ester(1403257-79-3)

Safety Data

• Hazardous Substances Data: 1403257-79-3(Hazardous Substances Data)

Usage

General Description

Benzoic acid, 5-bromo-3-[ethyl(tetrahydro-2H-pyran-4-yl)amino]-2-methyl-, methyl ester is a chemical compound with a complex structure. It contains a benzoic acid group along with a bromo, ethyl, and methyl groups connected to a 3-amino-2-methyl group. The compound is a methyl ester, meaning it has a carboxylic acid group that has been modified with a methyl group. This chemical is used in various industries such as pharmaceuticals, cosmetics, and research due to its diverse chemical properties and potential applications. It is important to handle this chemical with caution and ensure proper safety measures are in place when handling and using it.

Upstream product

• 1403257-49-7 2-methyl-3[(tetrahydro-2H-pyran-4-yl)amino]-5-bromobenzoic acid methyl ester 
• 75-07-0 acetaldehyde 
• 84302-42-1 2,3-dihydro-4H-pyran-4-one 
• 75-03-6 ethyl iodide 
• 1000342-11-9 2-methyl-3-amino-5-bromobenzoic acid methyl ester 
• 79669-49-1 5-bromo-2-methylbenzoic acid 
• 1975-50-4 2-methyl-3-nitrobenzic acid 
• 220514-28-3 5-bromo-2-methyl-3-nitrobenzoic acid methyl ester 
• 107650-20-4 5-bromo-2-methyl-3-nitro-benzoic acid 
• 29943-42-8 Tetrahydro-4H-pyran-4-one 

Downstream Products

• 1403254-99-8 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 
• 1403255-31-1 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-methyl-5-(6-(morpholinomethyl)pyridin-3-yl)benzamide 
• 1403258-05-8 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-5-(6-formylpyridin-3-yl)-2-methylbenzamide 
• 1403255-32-2 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-4'-((dimethylamino)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-[1,1'-biphenyl]-3-carboxamide 
• 1403258-06-9 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4'-formyl-4-methyl-[1,1'-biphenyl]-3-carboxamide 
• 1403255-83-3 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4'-(hydroxymethyl)-4-methyl-[1,1'-biphenyl]-3-carboxamide 
• 1403255-84-4 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide 
• 1403258-10-5 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-3'-formyl-4-methyl-[1,1'-biphenyl]-3-carboxamide 
• 1403255-91-3 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-3'-fluoro-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide 
• 1403258-20-7 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-3'-fluoro-4'-formyl-4-methyl-[1,1'-biphenyl]-3-carboxamide 
• 1403255-92-4 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2'-fluoro-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide 
• 1403258-21-8 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2'-fluoro-4'-formyl-4-methyl-[1,1'-biphenyl]-3-carboxamide 
• 1403255-93-5 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2',4-dimethyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide 
• 1403258-22-9 N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4'-formyl-2',4-dimethyl-[1,1'-biphenyl]-3-carboxamide 

Relevant articles and documents

Preparation Method for Amide Compounds and Use Thereof in Medical Field

Provided are a preparation method for amide compounds and use thereof in medical field. Specifically, provided are small molecule amide compounds. Such compounds are inhibitors of enhancer homolog 2 (EZH2) of Zeste gene, and can be used for preventing and/or treating related diseases mediated by EZH2, including tumors, myeloproliferative diseases or autoimmune diseases.

POLYSUBSTITUTED BENZENE COMPOUND AND PREPARATION METHOD AND USE THEREOF

The present invention provides a novel EZH2 inhibitor compound represented by formula (I) and a use of the inhibitor compound in preventing or treating a disease mediated by EZH2.

Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma

Traditional EZH2 inhibitors are developed to suppress the enzymatic methylation activity, and they may have therapeutic limitations due to the nonenzymatic functions of EZH2 in cancer development. Here, we report proteolysis-target chimera (PROTAC)-based EZH2 degraders to target the whole EZH2 in lymphoma. Two series of EZH2 degraders were designed and synthesized to hijack E3 ligase systems containing either von Hippel-Lindau (VHL) or cereblon (CRBN), and some VHL-based compounds were able to mediate EZH2 degradation. Two best degraders, YM181 and YM281, induced robust cell viability inhibition in diffuse large B-cell lymphoma (DLBCL) and other subtypes of lymphomas, outperforming a clinically used EZH2 inhibitor EPZ6438 (tazemetostat) that was only effective against DLBCL. The EZH2 degraders displayed promising antitumor activities in lymphoma xenografts and patient-derived primary lymphoma cells. Our study demonstrates that EZH2 degraders have better therapeutic activity than EZH2 inhibitors, which may provide a potential anticancer strategy to treat lymphoma.