848491-25-8

Basic information

• Product Name: 4-Quinazolinamine, N-(3-chloro-2,4-difluorophenyl)-7-methoxy-6-(4-piperidinyloxy)-
• CAS NO: 848491-25-8
• Molecular Formula: C20H19ClF2N4O2
• Molecular Weight: 420.846
• Mol File: 848491-25-8.mol
• Article Data: 3

Chemical Properties

• Boiling Point: 517.3±50.0 °C(Predicted)
• Density: 1.389±0.06 g/cm3(Predicted)
• CAS DataBase Reference: 4-Quinazolinamine, N-(3-chloro-2,4-difluorophenyl)-7-methoxy-6-(4-piperidinyloxy)-(CAS DataBase Reference)
• NIST Chemistry Reference: 4-Quinazolinamine, N-(3-chloro-2,4-difluorophenyl)-7-methoxy-6-(4-piperidinyloxy)-(848491-25-8)
• EPA Substance Registry System: 4-Quinazolinamine, N-(3-chloro-2,4-difluorophenyl)-7-methoxy-6-(4-piperidinyloxy)-(848491-25-8)

Safety Data

• Hazardous Substances Data: 848491-25-8(Hazardous Substances Data)

Upstream product

• 574745-97-4 4-chloro-6-hydroxy-7-methoxyquinazoline 
• 230955-75-6 6-acetoxy-4-chloro-7-methoxyquinazoline 
• 612501-45-8 tert-butyl 4-((4-chloro-7-methoxy-quinazolin-6-yl)oxy)piperidine-1-carboxylate 
• 2613-34-5 2,4-difluoro-3-chloro-aniline 

Relevant articles and documents

Discovery of AZD8931, an equipotent, reversible inhibitor of signaling by EGFR, HER2, and HER3 receptors

Deregulation of HER family signaling promotes proliferation and tumor cell survival and has been described in many human cancers. Simultaneous, equipotent inhibition of EGFR-, HER2-, and HER3-mediated signaling may be of clinical utility in cancer settings where the selective EGFR or HER2 therapeutic agents are ineffective or only modestly active. We describe the discovery of AZD8931 (2), an equipotent, reversible inhibitor of EGFR-, HER2-, and HER3-mediated signaling and the structure-activity relationships within this series. Docking studies based on a model of the HER2 kinase domain helped rationalize the increased HER2 activity seen with the methyl acetamide side chain present in AZD8931. AZD8931 exhibited good pharmacokinetics in preclinical species and showed superior activity in the LoVo tumor growth efficacy model compared to close analogues. AZD8931 is currently being evaluated in human clinical trials for the treatment of cancer.

QUINAZOLINE DERIVATIVES

The invention concerns quinazoline derivatives of Formula (I): wherein each of R1, R2, X1, R5 and m have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of EGF and erbB receptor tyrosine kinases.