Journal
NUCLEAR MEDICINE AND BIOLOGY
Volume 28, Issue 4, Pages 359-374Publisher
ELSEVIER SCIENCE INC
DOI: 10.1016/S0969-8051(01)00200-1
Keywords
EGFr; tyrosine kinase; quinazoline; biodistribution; fluorine-18; PET
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As PET candidate tracers for EGFr-TK, five 4-(anilino)quinazoline derivatives, each fluorinated in the aniline moiety, were prepared. Each was tested in vitro for inhibition of EGFr autophosphorylation in A431 cell line. The leading compounds were then radiolabeled with F-18 and cell binding experiments, biodistribution and PET studies in A431 tumor-bearing mice were performed. Metabolic studies were carried out in a mice control group. From our results, we concluded that while in vitro experiments indicates efficacy of 4-(anilino)quinazoline compounds, kinetic factors and rapid blood clearance make them unsuitable as tracers for nuclear medicine imaging of EGFr-TK. (C) 2001 Elsevier Science Inc. All rights reserved.
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