3-[(6,7-Dimethoxy-4-quinazolinyl)amino]-phenol (Janex 3; WHI-P180)
• potent inhibitor of IgE-mediated mast cell responses to allergens in vitro and in vivo. Also inhibits cyclin-dependent kinase 2 (CDK2; IC50 = 1µM) by blocking the ATP site
OTAVAchemicals Catalogue Number: 7015070102
CAS Registry Number: 211555-08-7
Purity: 95%+ (HPLC)
Ref. 1: Shewchuk et al. Binding mode of the 4-anilinoquinazoline class of protein kinase inhibitor: X-ray crystallographic studies of 4-anilinoquinazolines bound to cyclin-dependent kinase 2 and p38 kinase. Journal of Medicinal Chemistry (2000), 43, 133-138
Abstract: 4-Anilinoquinazolines represent an important class of protein kinase inhibitor. Modes of binding for two members of this inhibitor class were determined by x-ray of one inhibitor (4-[3-hydroxyanilino]-6,7-dimethoxyquinazoline) in complex with cyclin-dependent kinase 2 (CDK2) and the other (4-[3-methylsulfanylanilino]-6,7-dimethoxyquinazoline) in complex with p38 kinase.
Ref. 2: Chen et al. Pharmacokinetics and biologic activity of the novel mast cell inhibitor, 4-(3'-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline in mice. Pharmaceutical Research (1999), 16, 117-122
Abstract: The purpose of the present study was to examine the pharmacodynamic and pharmacokinetic features of the novel mast cell inhibitor 4-(3'-Hydroxyphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P180) in mice. Notably, WHI-P180, when administered in two consecutive nontoxic i.p. bolus doses of 25 mg/kg, inhibited IgE/antigen-induced vascular hyperpermeability in a well-characterized murine model of passive cutaneous anaphylaxis. WHI-P180 is an active inhibitor of IgE-mediated mast cell responses in vitro and in vivo. Further preclinical characterization of WHI-P180 may improve the efficacy of WHI-P180 in vivo and provide the basis for design of effective treatment and prevention programs for mast cell- mediated allergic reactions.