1033743-21-3

Basic information

• Product Name: 2-chloro-6-(3-(methylsulfonyl)phenyl)-4-morpholinothieno[3,2-d]pyrimidine
• Synonyms: 2-chloro-6-(3-(methylsulfonyl)phenyl)-4-morpholinothieno[3,2-d]pyrimidine
• CAS NO: 1033743-21-3
• Molecular Weight: 409.917
• Mol File: 1033743-21-3.mol

Chemical Properties

• CAS DataBase Reference: 2-chloro-6-(3-(methylsulfonyl)phenyl)-4-morpholinothieno[3,2-d]pyrimidine(CAS DataBase Reference)
• NIST Chemistry Reference: 2-chloro-6-(3-(methylsulfonyl)phenyl)-4-morpholinothieno[3,2-d]pyrimidine(1033743-21-3)
• EPA Substance Registry System: 2-chloro-6-(3-(methylsulfonyl)phenyl)-4-morpholinothieno[3,2-d]pyrimidine(1033743-21-3)

Safety Data

• Hazardous Substances Data: 1033743-21-3(Hazardous Substances Data)

Upstream product

• 956034-15-4 4-(2-chloro-6-iodothieno[3,2-d]pyrimidin-4-yl)morpholine 
• 373384-18-0 3-(methanesulfonyl)phenylboronic acid 

Downstream Products

• 1033736-84-3 5-(6-(3-(methylsulfonyl)phenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyridine-3-carboxylic acid 
• 1033736-15-0 5-(6-(3-(methylsulfonyl)phenyl)-4-morpholinothieno[3,2-d]pyrimidin-2-yl)pyrimidin-2-amine 

Relevant articles and documents

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor

Efforts to identify potent small molecule inhibitors of PI3 kinase and mTOR led to the discovery of the exceptionally potent 6-aryl morpholino thienopyrimidine 6. In an effort to reduce the melting point in analogs of 6, the thienopyrimidine was modified by the addition of a methyl group to disrupt planarity. This modification resulted in a general improvement in in vivo clearance. This discovery led to the identification of GNE-477 (8), a potent and efficacious dual PI3K/mTOR inhibitor.

PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND METHODS OF USE

Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. Formula (Ic) and (Id).

PHOSPHOINOSITIDE 3-KINASE INHIBITOR COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Compounds of Formulas (Ia) and (Ib), and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula (Ia) and (Ib) for in vitro, in situ, and in vivodiagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.