35265-88-4

Basic information

• Product Name: Thieno[3,2-d]pyriMidine, 2-chloro-7-Methyl-4-(4-Morpholinyl)-
• Synonyms: Thieno[3,2-d]pyriMidine, 2-chloro-7-Methyl-4-(4-Morpholinyl)-;2-Chloro-7-methyl-4-(4-morpholinyl)thieno[3,2-d]pyrimidine;Thieno[3,2-d]pyriMidine, 2-chloro-7-Methyl-4-(4-Morpholinyl)-4;4-(2-chloro-7-methylthieno[3,2-d]pyrimidin-4-yl)morpholine
• CAS NO: 35265-88-4
• Molecular Formula: C11H12ClN3OS
• Molecular Weight: 269.75048
• Mol File: 35265-88-4.mol
• Article Data: 5

Chemical Properties

• Appearance: /
• Storage Temp.: under inert gas (nitrogen or Argon) at 2–8 °C
• CAS DataBase Reference: Thieno[3,2-d]pyriMidine, 2-chloro-7-Methyl-4-(4-Morpholinyl)-(CAS DataBase Reference)
• NIST Chemistry Reference: Thieno[3,2-d]pyriMidine, 2-chloro-7-Methyl-4-(4-Morpholinyl)-(35265-88-4)
• EPA Substance Registry System: Thieno[3,2-d]pyriMidine, 2-chloro-7-Methyl-4-(4-Morpholinyl)-(35265-88-4)

Safety Data

• Hazardous Substances Data: 35265-88-4(Hazardous Substances Data)

Usage

General Description

Thieno[3,2-d]pyriMidine, 2-chloro-7-Methyl-4-(4-Morpholinyl)- is a chemical compound with the molecular formula C13H15ClN4O. It is a heterocyclic compound containing a thieno and pyrimidine ring structure, with a 2-chloro, 7-methyl, and 4-(4-morpholinyl) substituents. Thieno[3,2-d]pyriMidine, 2-chloro-7-Methyl-4-(4-Morpholinyl)- is used in pharmaceutical research and drug development, particularly in the development of potential drugs for the treatment of various medical conditions. Its unique structure and properties make it a potentially valuable compound for the development of new medications with therapeutic applications.

Upstream product

• 110-91-8 morpholine 
• 35265-83-9 2,4-dichloro-7-methyl-thieno[3,2-d]pyrimidine 
• 85006-31-1 3-amino-4-methyl-2-thiophenecarboxylic acid methyl ester 
• 35265-81-7 7-methylthieno<3,2-d>pyrimidine-2,4-dione 

Downstream Products

• 955979-02-9 2-chloro-7-methyl-4-morpholinothieno[3,2-d]-pyrimidine-6-carbaldehyde 
• 1394076-92-6 GNE-317 
• 1394077-00-9 4-(2-chloro-6-(3-methoxyoxetan-3-yl)-7-methylthieno[3,2-d]pyrimidin-4-yl)morpholine 
• 1032757-09-7 (R)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one 

Relevant articles and documents

Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer

PARP inhibitors have achieved great success in cancers with BRCA mutations, but only a small portion of patients carry BRCA mutations, which results in their narrow indication spectrum. Recently, emerging evidence has demonstrated that combinations of PARP and PI3K inhibitors could evoke unanticipated synergistic effects in various cancers, even including BRCA-proficient ones. In this work, a series of PARP/PI3K dual inhibitors were designed, synthesized, and evaluated for their biological activities. It was found that compounds 9a and 23a exhibited excellent inhibitory activities against PARP-1 (9a: IC50 = 1.57 nM, 23a: IC50 = 0.91 nM) and PI3Kα (9a: IC50 = 2.0 nM, 23a: IC50 = 1.5 nM), and showed promising antiproliferative activities against both BRCA-deficient (HCT-116, HCC-1937) and BRCA-proficient (SW620, MDA-MB-231/468) tumor cells. 9a and 23a also exhibited considerable in vivo antitumor efficacy in an MDA-MB-468 xenograft mouse model, with TGI values of 56.39% and 48.77%, respectively. Additionally, 23a possessed promising profiles including high kinase selectivity and low cardiotoxicity. Overall, this work indicates 9a and 23a might be potential PARP/PI3K dual inhibitors for cancer therapy and deserve further research.

PROCESS FOR MAKING THIENOPYRIMIDINE COMPOUNDS

Process methods for making the dual mTOR/PI3K inhibitor GDC-0980, named as (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, having the structure: and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof.

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).