1445993-87-2

Basic information

• Product Name: 4-bromo-6-methyl-1-tosyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-one
• Synonyms: 4-bromo-6-methyl-1-tosyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-one;4-bromo-6-methyl-1-(4-methylbenzenesulfonyl)-1H,6H,7H-pyrrolo[2,3-c]pyridin-7-one
• CAS NO: 1445993-87-2
• Molecular Formula: C₁₅H₁₃BrN₂O₃S
• Molecular Weight: 381.24432
• Mol File: 1445993-87-2.mol
• Article Data: 27

Chemical Properties

• Boiling Point: 564.2±60.0 °C(Predicted)
• Appearance: /
• Density: 1.59±0.1 g/cm3(Predicted)
• PKA: -4.40±0.40(Predicted)
• CAS DataBase Reference: 4-bromo-6-methyl-1-tosyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-one(CAS DataBase Reference)
• NIST Chemistry Reference: 4-bromo-6-methyl-1-tosyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-one(1445993-87-2)
• EPA Substance Registry System: 4-bromo-6-methyl-1-tosyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-one(1445993-87-2)

Safety Data

• Hazardous Substances Data: 1445993-87-2(Hazardous Substances Data)

Usage

General Description

4-bromo-6-methyl-1-tosyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-one is a chemical compound with the molecular formula C16H14BrNO3S. It is a tosyl derivative of a pyrrolopyridine compound, featuring a bromine atom at the 4-position and a methyl group at the 6-position. 4-bromo-6-methyl-1-tosyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-one is known for its potential pharmaceutical applications, particularly in the fields of medicinal chemistry and drug development. Its unique structure and functional groups make it a valuable building block for the synthesis of new bioactive compounds. Studies have shown that derivatives of 1H-pyrrolo[2,3-c]pyridin-7(6H)-one exhibit a range of biological activities, including antiviral, anticancer, and antimicrobial properties, making them promising candidates for further investigation and potential therapeutic use.

Upstream product

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• 1622303-42-7 (E)-5-bromo-4-(2-(dimethylamino)vinyl)-1-methyl-3-nitropyridin-2(1H)-one 
• 1446237-40-6 5-bromo-1,4-dimethyl-3-nitro-1,2-dihydropyridin-2-one 
• 228410-90-0 2-hydroxy-5-bromo-4-methyl-3-nitropyridine 
• 100367-40-6 2-amino-3-nitro-4-methyl-5-bromopyridine 
• 6635-86-5 2-amino-4-methyl-3-nitropyridine 
• 1361481-63-1 4-bromo-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one 
• 98-59-9 p-toluenesulfonyl chloride 
• 1258960-27-8 4-bromo-7-chloro-1-p-toluenesulfonyl-1H-pyrrolo[2,3-c]pyridine 
• 67443-38-3 5-bromo-2-chloro-3-nitropyridine 
• 425380-38-7 4-bromo-7-chloro-3a,7a-dihydro-1H-pyrrolo[2,3-c]pyridine 
• 1445993-86-1 4-bromo-1-[(4-methylphenyl)sulfonyl]-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one 

Downstream Products

• 1446232-71-8 N-[3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(tetrahydro-2H-pyran-4-yloxy)phenyl]propane-1-sulfonamide 
• 1446232-72-9 2,2,2-trifluoro-N-[3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(tetrahydro-2H-pyran-4-yloxy)phenyl]ethanesulfonamide 
• 1445992-74-4 ethyl 3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxybenzoate 
• 1445992-76-6 3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxybenzoic acid 
• 1445992-82-4 N-ethyl-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxybenzamide 
• 1445992-84-6 3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxy-N-(tetrahydrofuran-2-ylmethyl)benzamide 
• 1445993-93-0 3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxybenzoyl chloride 
• 1445994-30-8 4-(5-amino-2-(tetrahydro-2H-pyran-4-yloxy)phenyl)-6-methyl-1H-pyrrolo[2,3-c]pyridin-7(6H)-one 
• 1445993-30-5 ethyl 4-(cyclopentylamino)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)benzoate 
• 1445992-63-1 6-methyl-4-(5-nitro-2-phenoxyphenyl)-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one 
• 1445993-94-1 6-methyl-4-(5-nitro-2-(tetrahydro-2H-pyran-4-yloxy)phenyl)-1H-pyrrolo[2,3-c]pyridin-7(6H)-one 
• 1445992-64-2 4-(5-amino-2-phenoxyphenyl)-6-methyl-1,6-dihydro-7H-pyrrolo[2,3-c]pyridin-7-one 
• 1445992-65-3 N-[3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxyphenyl]methanesulfonamide 
• 1445992-66-4 2,2,2-trifluoro-N-[3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxyphenyl]ethanesulfonamide 

Relevant articles and documents

Antibody Conjugation of a Chimeric BET Degrader Enables in vivo Activity

The ability to selectively degrade proteins with bifunctional small molecules has the potential to fundamentally alter therapy in a variety of diseases. However, the relatively large size of these chimeric molecules often results in challenging physico-chemical properties (e. g., low aqueous solubility) and poor pharmacokinetics which may complicate their in vivo applications. We recently discovered an exquisitely potent chimeric BET degrader (GNE-987) which exhibited picomolar cell potencies but also demonstrated low in vivo exposures. In an effort to improve the pharmacokinetic properties of this molecule, we discovered the first degrader-antibody conjugate by attaching GNE-987 to an anti-CLL1 antibody via a novel linker. A single IV dose of the conjugate afforded sustained in vivo exposures that resulted in antigen-specific tumor regressions. Enhancement of a chimeric protein degrader with poor in vivo properties through antibody conjugation thereby expands the utility of directed protein degradation as both a biological tool and a therapeutic possibility.

BRD4 inhibitor as well as a preparative method and use thereof

The compound of formula (I) has a good inhibitory effect on the proliferation of human prostate cancer cells CWR22RV1 and breast cancer cells; and combined use of the compound with an androgen receptor inhibitor HC-1119 significantly enhances the inhibitory effect on prostate cancer cells, and the inhibitory effect increases with increased concentration. The compound of formula (I) can not only be used independently to prepare an antineoplastic agent but can also be used in combination with other agents having antineoplastic effects, such as an androgen receptor inhibitor, or other targeting drugs etc., to prepare an antineoplastic agent having stronger therapeutic effects, especially an agent for treating prostate cancer and breast cancer.

BET INHIBITORS FOR MODULATING DUX4 EXPRESSION IN FSHD

The present disclosure provides BET inhibitors of the formula: wherein the variables are defined herein, as well as pharmaceutical compositions thereof. The present disclosure also provides methods of treating a patient comprising administering a bromo- and extra-terminal (BET) domain inhibitor for the treatment of FSHD which modulates DUX4 expression. In some embodiments, the present methods comprise using one or more BET inhibitors as a therapeutic agent for the treatment of FSHD patients including patients who are being treated with one or more palliative treatments such as therapy and/or agents which lead to increased muscle mass.