1421373-50-3

Basic information

• Product Name: N-(5-((5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methylpiperazin-1-yl)phenyl)acrylamide
• Synonyms: N-(5-((5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methylpiperazin-1-yl)phenyl)acrylamide
• CAS NO: 1421373-50-3
• Molecular Weight: 519.006
• Mol File: 1421373-50-3.mol
• Article Data: 3

Chemical Properties

• CAS DataBase Reference: N-(5-((5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methylpiperazin-1-yl)phenyl)acrylamide(CAS DataBase Reference)
• NIST Chemistry Reference: N-(5-((5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methylpiperazin-1-yl)phenyl)acrylamide(1421373-50-3)
• EPA Substance Registry System: N-(5-((5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methylpiperazin-1-yl)phenyl)acrylamide(1421373-50-3)

Safety Data

• Hazardous Substances Data: 1421373-50-3(Hazardous Substances Data)

Upstream product

• 1421372-30-6 5-chloro-N-(2-methoxy-4-(4-methylpiperazin-1-yl)-5-nitrophenyl)-4-(pyrazolo[1,5-a]pyridin-3-yl)pyrimidin-2-amine 
• 1421372-29-3 N'-(5-chloro-4-(pyrazolo[1,5-a]pyridin-3-yl)pyrimidin-2-yl)-4-methoxy-6-(4-methylpiperazine-1-yl)benzene-1,3-diamine 
• 814-68-6 acryloyl chloride 
• 1075705-01-9 4-fluoro-2-methoxy-5-nitro-phenylamine 
• 1224708-12-6 4-[(E)-2-butoxyethenyl]-2,5-dichloropyrimidine 
• 1224709-13-0 3-(2,5-dichloropyrimidin-4-yl)pyrazolo[1,5-a]pyridine 
• 1421372-08-8 5-chloro-N-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(pyrazolo[1,5-a]pyridin-3-yl)pyrimidin-2-amine 
• 450-91-9 4-fluoro-2-methoxyaniline 

Relevant articles and documents

HETEROARYL COMPOUNDS FOR KINASE INHIBITION

Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFRand mutant HER2 activity, are described herein.

Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR)

A novel series of small-molecule inhibitors has been developed to target the double mutant form of the epidermal growth factor receptor (EGFR) tyrosine kinase, which is resistant to treatment with gefitinib and erlotinib. Our reported compounds also show selectivity over wild-type EGFR. Guided by molecular modeling, this series was evolved to target a cysteine residue in the ATP binding site via covalent bond formation and demonstrates high levels of activity in cellular models of the double mutant form of EGFR. In addition, these compounds show significant activity against the activating mutations, which gefitinib and erlotinib target and inhibition of which gives rise to their observed clinical efficacy. A glutathione (GSH)-based assay was used to measure thiol reactivity toward the electrophilic functionality of the inhibitor series, enabling both the identification of a suitable reactivity window for their potency and the development of a reactivity quantitative structure-property relationship (QSPR) to support design.