1372540-25-4

Basic information

• Product Name: GSK2636771
• Synonyms: GSK2636771;2-Methyl-1-[[2-Methyl-3-(trifluoroMethyl)phenyl]Methyl]-6-(4-Morpholinyl)-1H-benziMidazole-4-carboxylic acid;GSK2636771/GSK-2636771;1H-Benzimidazole-4-carboxylic acid, 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(4-morpholinyl)-;2-Methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid GSK2636771;GSK 2636771 dihydrochloride;2-Methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic;2-METHYL-1-[[2-METHYL-3-(TRIFLUOROMETHYL)PHENYL]METHYL]-6-MORPHOLIN-4-YLBENZIMIDAZOLE-4-CARBOXYLIC ACID
• CAS NO: 1372540-25-4
• Molecular Formula: C₂₂H₂₂F₃N₃O₃
• Molecular Weight: 433.4235896
• Product Categories: PI3K/Akt/mTOR;Inhibitors;Akt;mTOR;PI3K
• Mol File: 1372540-25-4.mol
• Article Data: 4

Chemical Properties

• Boiling Point: 641.3±55.0 °C(Predicted)
• Appearance: /
• Density: 1.38
• Storage Temp.: -20°C Freezer
• Solubility: DMSO (Slightly), Methanol (Slightly)
• PKA: -2.70±0.30(Predicted)
• CAS DataBase Reference: GSK2636771(CAS DataBase Reference)
• NIST Chemistry Reference: GSK2636771(1372540-25-4)
• EPA Substance Registry System: GSK2636771(1372540-25-4)

Safety Data

• Hazardous Substances Data: 1372540-25-4(Hazardous Substances Data)

Usage

Description

GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor that is particularly sensitive to PTEN null cell lines. It is a pharmaceutical compound designed to target the PI3Kβ isoform of the phosphoinositide 3-kinase (PI3K) pathway, which plays a crucial role in cellular processes such as cell growth, proliferation, and survival. The selective inhibition of PI3Kβ by GSK2636771 makes it a promising candidate for the development of targeted therapies in various diseases.

Uses

Used in Oncology:
GSK2636771 is used as an oncology agent for the treatment of cancer. Its PI3Kβ-selective inhibition is particularly effective in PTEN null cell lines, which are often associated with aggressive and treatment-resistant forms of cancer. By targeting the PI3Kβ pathway, GSK2636771 can potentially inhibit tumor growth and proliferation, making it a valuable tool in the fight against cancer.
Used in Drug Development:
GSK2636771 is also used in the development of novel drug delivery systems and therapeutic strategies. Its PI3Kβ-selective inhibition property can be leveraged to design targeted drug delivery systems that specifically release the compound in cancer cells, thereby improving its bioavailability and therapeutic outcomes. Additionally, GSK2636771 can be studied in combination with other chemotherapeutic agents to explore synergistic effects and enhance the overall efficacy of cancer treatment.

Upstream product

• 1372540-24-3 methyl 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylate 
• 2516-95-2 5-chloro-2-nitrobenzoic acid 
• 1372540-21-0 methyl 2-methyl-5-(4-morpholinyl)-1H-benzimidazole-7-carboxylate 
• 1203486-58-1 methyl 3-amino-5-(4-morpholinyl)-2-nitrobenzoate 
• 874301-23-2 3-amino-5-chloro-2-nitrobenzoic acid methyl ester 

Downstream Products

• 1372540-91-4 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid 2-amino-2-(hydroxymethyl)-1,3-propanediol salt 
• 1372540-93-6 ethyl 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylate 
• 1372540-34-5 C₂₂H₂₁ClF₃N₃O₂ 
• 1372540-32-3 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-4-(4H-1,2,4-triazol-3-yl)-1H-benzimidazole 
• 1372540-33-4 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxamide 

Relevant articles and documents

COMBINATION TREATMENT FOR CANCER

Disclosed herein is a method of treatment involving the combination of an OX40 antigen binding protein (e.g., an anti-OX40 agonist antibody) and a PI3Kb inhibitor for use in treating a cancer, such as a PTEN deficient cancer.

COMBINATION DRUG THERAPY

A novel combination comprising the androgen receptor inhibitor, 4-(3-(4-Cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide or a pharmaceutically acceptable salt or solvate thereof, with a PI3K? inhibitor, 2-methyl-1-{[2-methyl-3-(trifluoromethyl)phenyl]methyl}-6-(4-morpholinyl)-1H-benzimidazole-4-carboxylic acid, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of androgen receptor and/or PI3K? is beneficial, e.g., cancer.