1421357-83-6

Basic information

• Product Name: (S)-(2-methoxy-5-(4-(3-methylmorpholine)-2-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7-yl)phenyl)methanol
• Synonyms: (S)-(2-methoxy-5-(4-(3-methylmorpholine)-2-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7-yl)phenyl)methanol
• CAS NO: 1421357-83-6
• Molecular Weight: 450.538
• Mol File: 1421357-83-6.mol

Chemical Properties

• CAS DataBase Reference: (S)-(2-methoxy-5-(4-(3-methylmorpholine)-2-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7-yl)phenyl)methanol(CAS DataBase Reference)
• NIST Chemistry Reference: (S)-(2-methoxy-5-(4-(3-methylmorpholine)-2-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7-yl)phenyl)methanol(1421357-83-6)
• EPA Substance Registry System: (S)-(2-methoxy-5-(4-(3-methylmorpholine)-2-(tetrahydro-2H-pyran-4-yl)pyrido[2,3-d]pyrimidin-7-yl)phenyl)methanol(1421357-83-6)

Safety Data

• Hazardous Substances Data: 1421357-83-6(Hazardous Substances Data)

Upstream product

• 1421357-84-7 (S)-(5-(2-(3,6-dihydro-2H-pyran-4-yl)-4-(3-methylmorpholinyl)pyrido[2,3-d]pyrimidine-7-yl)2-methoxyphenyl)methanol 
• 1009303-74-5 (S)-(5-(2-chloro-4-(3-methylmorpholinyl)pyrido[2,3-d]pyrimidin-7-yl)-2-methoxyphenyl)methanol 
• 287944-16-5 4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-3,6-dihydro-2H-pyran 
• 535924-69-7 tributyl(3,6-dihydro-2H-pyran-4-yl)stannane 

Relevant articles and documents

Design and synthesis of alkyl substituted pyridino[2,3-D]pyrimidine compounds as PI3Kα/mTOR dual inhibitors with improved pharmacokinetic properties and potent in vivo antitumor activity

Using pyridino[2,3-D]pyrimidine as the core, total 13 pyridino[2,3-D]pyrimidine derivatives with different alkyl substituents at C2 site have been designed and synthesized to search for novel PI3Kα/mTOR dual inhibitors. Most of the target compounds showed potent mTOR inhibition activity with IC50 values ranging from single to double digit nanomole. Five target compounds exhibited pronounced PI3Kα inhibition activity. In vitro cellular assay indicated that most of the target compounds showed excellent antiproliferative activity, especially 3j whose potency against SKOV3 was 8-fold higher than the positive control AZD8055. In vitro metabolic stability study found that 3j had a comparable stability to that of AZD8055. More importantly, 3j showed better antitumor activity and pharmacokinetic properties in vivo as compared with AZD8055.

Pyridine and miazines mTOR inhibitors

The invention belongs to the technical field of medicines, and particularly relates to a pyridopyrimidine mammalian target of rapamycin (mTOR) inhibitor which is shown as a general formula (I), pharmaceutically acceptable salts and stereoisomers thereof, and deuterated pyridopyrimidine mammalian mTOR inhibitors, wherein Z, Z, Z, R, R, R, X and W are defined in the specifications. The invention also relates to preparation methods for the compounds, medicinal inhibitors and medicinal compositions which contain the compounds, and the application of the compounds to preparation of medicines for treating and/or preventing post-transplant lymphoproliferative diseases which have response to inhibition of mTOR activity.