1086062-66-9

Basic information

• Product Name: GSK-2126458
• Synonyms: GSK2126458;GSK-2126458;2,4-Difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]benzenesulfonamide;GSK212;2,4-Difluoro-N-[2-Methoxy-5-[4-(pyridazin-4-yl)quinolin-6-yl]pyridin-3-yl]benzenesulfonaMide;GSK2126458 (GSK458);OMipalisib;GSK458
• CAS NO: 1086062-66-9
• Molecular Formula: C₂₅H₁₇F₂N₅O₃S
• Molecular Weight: 505.4959864
• EINECS: -0
• Product Categories: Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;PI3K/Akt/mTOR;Inhibitors;Akt;mTOR;PI3K
• Mol File: 1086062-66-9.mol
• Article Data: 2

Chemical Properties

• Melting Point: 187-189℃
• Boiling Point: 715.6±70.0 °C(Predicted)
• Appearance: /
• Density: 1.45
• Storage Temp.: Refrigerator
• Solubility: Chloroform (Slightly), DMSO (Slightly), Methanol (Very Slightly, Heated)
• PKA: 6.23±0.40(Predicted)
• CAS DataBase Reference: GSK-2126458(CAS DataBase Reference)
• NIST Chemistry Reference: GSK-2126458(1086062-66-9)
• EPA Substance Registry System: GSK-2126458(1086062-66-9)

Safety Data

• Hazardous Substances Data: 1086062-66-9(Hazardous Substances Data)

Usage

Description

GSK2126458 is a potent inhibitor of phosphoinositide 3-kinase (PI3K) isoforms and the mammalian target of Rapamycin (mTOR), with high selectivity and affinity for its targets. It is orally bioavailable, displays favorable pharmacokinetics, and shows efficacy in tumor growth models. GSK2126458 also positively combines with inhibitors of discoidin domain receptor 1 (DDR1) to suppress the growth of certain cancer cells.

Uses

Used in Pharmaceutical Industry:
GSK2126458 is used as a highly potent inhibitor for the treatment of cancer. It targets the PI3K and mTOR pathways, which play a crucial role in cell growth, proliferation, and survival. By inhibiting these pathways, GSK2126458 can effectively suppress tumor growth and has potential applications in the treatment of various cancer types.
Used in Cancer Research:
GSK2126458 is used as a research tool to study the role of PI3K and mTOR in cancer development and progression. It helps researchers understand the molecular mechanisms underlying the regulation of these pathways and their contribution to cancer growth, providing valuable insights for the development of novel therapeutic strategies.
Used in Drug Combination Therapy:
GSK2126458 is used in combination with other cancer treatments, such as DDR1 inhibitors, to enhance the therapeutic efficacy and overcome drug resistance in cancer treatment. This combination approach can lead to improved outcomes for patients with advanced or resistant cancers.

Upstream product

• 1086063-46-8 N-(5-bromo-2-methoxypyridine-3-yl)-2,4-difluorobenzene sulfonyl chloride 
• 1086063-18-4 6-bromo-4-(pyridazin-4-yl)quinoline 
• 152684-30-5 5-bromo-2-methoxy-3-nitropyridine 
• 15862-34-7 5-bromo-3-nitro-2-pyridone 
• 67443-38-3 5-bromo-2-chloro-3-nitropyridine 
• 884495-39-0 5-bromo-2-(methyloxy)-3-pyridinamine 
• 1086062-75-0 6-bromo-4-chloroquinoline hydrochloride 
• 927801-23-8 6-bromo-4-iodoquinoline 
• 65340-70-7 6-bromo-4-chloroquinoline 
• 187278-01-9 5-(((4-bromophenyl)amino)methylene)-2,2-dimethyl-1,3-dioxane-4,6-dione 
• 145369-94-4 6-bromo-3-quinolinecarboxylic acid-4-ol 

Downstream Products

• 1360537-73-0 2,4-difluoro-N-(2-hydroxy-5-(4-(pyridazin-4-yl)quinolin-6-yl)pyridin-3-yl)benzenesulfonamide 

Relevant articles and documents

METHOD OF ADMINISTRATION AND TREATMENT

The present invention provides a method of treating a human with cancer comprising detecting at least one mutation in a PIK3CA gene or at least one mutant protein encoded by said PIK3CA gene from at least one first sample from said human and administering to said human an effective amount of 2,4-difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide or a pharmaceutically acceptable salt thereof in a pharmaceutical composition if said at least one sample has at least one mutant PI3K protein or a mutation in the PIK3CA gene.