1012057-31-6

Basic information

• Product Name: 4-((3-ethynylphenyl)amino)quinazolin-6-ol
• Synonyms: 4-((3-ethynylphenyl)amino)quinazolin-6-ol
• CAS NO: 1012057-31-6
• Molecular Weight: 261.283
• Mol File: 1012057-31-6.mol

Chemical Properties

• CAS DataBase Reference: 4-((3-ethynylphenyl)amino)quinazolin-6-ol(CAS DataBase Reference)
• NIST Chemistry Reference: 4-((3-ethynylphenyl)amino)quinazolin-6-ol(1012057-31-6)
• EPA Substance Registry System: 4-((3-ethynylphenyl)amino)quinazolin-6-ol(1012057-31-6)

Safety Data

• Hazardous Substances Data: 1012057-31-6(Hazardous Substances Data)

Upstream product

• 1012057-30-5 4-(3-ethynylphenylamino)quinazolin-6-yl acetate 
• 179688-15-4 3,4-dihydro-4-oxoquinazolin-6-yl acetate 
• 54060-30-9 3-acetylenephenylamine 
• 16064-10-1 6-hydroxyquinazolin-4(3H)-one 

Relevant articles and documents

TARTRATE SALTS OF QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY

The present invention relates to tartrate salts of quinazoline containing zinc-binding moiety based derivatives that are inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The tartrate salts may further act as HDAC inhibitors.

FORMULATION OF QUINAZOLINE BASED EGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY

The present invention relates to a composition comprising an inclusion complex of a cyclodextrin and quinazoline containing zinc-binding moiety based derivatives. The cyclodextrin is preferable a β-cyclodextrin or a derivative thereof. The quinazolines have enhanced and unexpected properties as inhibitors of epidermal growth factor receptor tyrosine kinase (EGFR-TK) and their use in the treatment of EGFR-TK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.

MULTI-FUNCTIONAL SMALL MOLECULES AS ANTI-PROLIFERATIVE AGENTS

The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.

Synthesis and SAR of potent EGFR/erbB2 dual inhibitors

A series of 6-alkoxy-4-anilinoquinazoline compounds was prepared and evaluated for in vitro inhibition of the erbB2 and EGFR kinase activity. The IC50 values of the best compounds were below 0.10 uM. Further, several of these compounds inhibit the growth of erbB2 and EGFR over-expressing tumor cell lines at concentrations below 1 uM.