Preclinical analysis of the analinoquinazoline AG1478, a specific small molecule inhibitor of EGF receptor tyrosine kinase

The tyrphostin 4-(3-chloroanilino)-6,7-dimethoxyquinazoline (AG1478) is a potent and specific inhibitor of EGFR tyrosine kinase whose favourable preclinical profile supports progression towards clinical trials. Microphysiometric evaluation revealed a short (10 μM were achieved over the duration of t...

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Veröffentlicht in:	Biochemical pharmacology 2006-05, Vol.71 (10), p.1422-1434
Hauptverfasser:	Ellis, A.G., Doherty, M.M., Walker, F., Weinstock, J., Nerrie, M., Vitali, A., Murphy, R., Johns, T.G., Scott, A.M., Levitzki, A., McLachlan, G., Webster, L.K., Burgess, A.W., Nice, E.C.
Format:	Artikel
Sprache:	eng
Schlagworte:	AG1478 Animals Area Under Curve Biological and medical sciences Cell Line, Tumor Dose-Response Relationship, Drug EGFR receptor Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Glioblastoma - drug therapy Glioblastoma - metabolism Glioblastoma - pathology Humans Injections, Intravenous Injections, Subcutaneous Medical sciences Mice Microphysiometer Molecular Structure Pharmacokinetics Pharmacology. Drug treatments Protein Tyrosine Phosphatases - antagonists & inhibitors Quinazoline Quinazolines Rats Receptor, Epidermal Growth Factor - antagonists & inhibitors Thymidine - metabolism Tyrosine kinase inhibitor Tyrphostins - chemistry Tyrphostins - pharmacokinetics Tyrphostins - pharmacology Xenograft Model Antitumor Assays
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