1083326-05-9

Basic information

• Product Name: N-(5-broMo-2-Methoxypyridin-3-yl)cyclopropanesulfonaMide
• Synonyms: N-(5-broMo-2-Methoxypyridin-3-yl)cyclopropanesulfonaMide;N-(5-bromo-2-methoxy-3-pyridinyl)cyclopropanesulfonamide
• CAS NO: 1083326-05-9
• Molecular Formula: C₉H₁₁BrN₂O₃S
• Molecular Weight: 307.16424
• Mol File: 1083326-05-9.mol
• Article Data: 16

Chemical Properties

• Appearance: /
• Storage Temp.: 2-8°C
• CAS DataBase Reference: N-(5-broMo-2-Methoxypyridin-3-yl)cyclopropanesulfonaMide(CAS DataBase Reference)
• NIST Chemistry Reference: N-(5-broMo-2-Methoxypyridin-3-yl)cyclopropanesulfonaMide(1083326-05-9)
• EPA Substance Registry System: N-(5-broMo-2-Methoxypyridin-3-yl)cyclopropanesulfonaMide(1083326-05-9)

Safety Data

• Hazardous Substances Data: 1083326-05-9(Hazardous Substances Data)

Upstream product

• 15862-34-7 5-bromo-3-nitro-2-pyridone 
• 6945-68-2 5-bromo-3-nitro-pyridin-2-ylamine 
• 1072-97-5 5-bromo-2-pyridylamine 
• 67443-38-3 5-bromo-2-chloro-3-nitropyridine 
• 152684-30-5 5-bromo-2-methoxy-3-nitropyridine 
• 884495-39-0 5-bromo-2-(methyloxy)-3-pyridinamine 
• 139631-62-2 cyclopropanesulfonyl chloride 

Downstream Products

• 1083325-77-2 N-{2-(methyloxy)-5-[3-(4-{[2-(methyloxy)phenyl]sulfonyl}-1-piperazinyl)-6-quinoxalinyl]-3-pyridinyl}cyclopropanesulfonamide 
• 1366129-44-3 N-[5-{2-amino-3-[4-(ethylsulfonyl)phenyl]-6-quinolinyl}-2-(methyloxy)-3-pyridinyl]cyclopropanesulfonamide 
• 1083326-71-9 N-(2-methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-pyridin-3-yl)cyclopropanesulfonamide 

Relevant articles and documents

Alkylsulfonamide-containing quinazoline derivatives as potent and orally bioavailable PI3Ks inhibitors

Phosphoinositide 3-kinases (PI3Ks) are regarded as promising targets for treatment of various cancers due to their roles in regulating cell proliferation, differentiation, migration, and survival. Here we report our efforts to develop potent and orally bioavailable PI3K inhibitors for the treatment of cancers. The alkylsulfonamide-containing quinazoline derivatives A1–A18 significantly inhibited PI3Kα, and cell proliferation among HCT-116, MCF-7 and SU-DHL-6 cell lines. The optimal compound A1 displayed potent inhibitory activity against PI3Kα (IC50 = 4.5 nM), PI3Kβ (IC50 = 4.5 nM), PI3Kγ (IC50 = 4.5 nM), PI3Kδ (IC50 = 4.5 nM) and significantly inhibited the growth of HCT-116, MCF-7 and SU-DHL-6 cell lines with IC50 values of 0.82 μM, 0.99 μM and 0.19 μM, respectively. Western blot analysis demonstrated A1 significantly suppressed the phosphorylation of AKTS473 in a dose-dependent manner. Furthermore, A1 could markedly inhibit cancer growth at the dose of 25 mg/kg in nude mouse HCT-116 xenograft model in vivo without causing significant weight loss or toxicity.

Discovery of new thienopyrimidine derivatives as potent and orally efficacious phosphoinositide 3-kinase inhibitors

A series of new thienopyrimidine derivatives has been discovered as potent PI3K inhibitors. The systematic SAR studies for these analogues are described. Among them, 8a and 9a exhibit nanomolar enzymatic potencies and sub-micromolar cellular anti-prolifer

6-(Pyridine-4-yl)-4-substituted amino quinazoline or quinoline compound and application thereof

The invention relates to 6-(pyridine-4-yl)-4-substituted amino quinazoline and quinoline compounds having PI3K inhibitory activity, which are compounds of formula (I) structure (as shown in the description), or solvates, enantiomers, diastereoisomers, tautomers or any-ratio mixtures of their pharmaceutically acceptable salts, including racemic mixtures. The 6-(pyridine-4-yl)-4-substituted amino quinazoline and quinoline compounds have good inhibitory action against PI3K, show good antitumor effect, and has a good prospect in the preparation of drugs for treatment of diseases responsive to PI3Kalpha and/or PI3K delta. The invention also relates to pharmaceutical application of the compounds as PI3K inhibitors.