title: Assessment of 11C-labeled-4-N-(3-bromoanilino)-6,7-dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression.
abstract: The aim of the present study was to investigate the biodistribution of (11)C-labeled-4-N-(3-bromoanilino), 6,7-dimethoxyquinazoline ((11)C-PD153035) and the relationship between accumulation of the tracer and epidermal growth factor receptor (EGFR) expression levels. Biodistribution studies of (11)C-PD153035 were performed in tumor-bearing nude mice. The amount of radioactivity in the lungs was small while concentrations were highest in the liver and intestine. From in vitro studies, the level of (11)C-PD153035 accumulation was detected in MDA-MB-468, A549, and MDA-MB-231 cells. The uptake of (11)C-PD153035 in cells was closely correlated with the EGFR expression level of cells (r(2) = 0.85; P < 0.001), and the results obtained in excised tumors were also significantly correlated (r(2) = 0.63; P = 0.003). Binding in MDA-MB-468, A549, and MDA-MB-231 tumors was reduced to background level at 60 min post injection( 11)C-PD153035 by pretreatment with cold PD153035. The present study showed that whether in vitro or ex vivo the uptake of (11)C-PD153035 closely correlated with EGFR expression levels. In contrast, blocking studies revealed specific binding in the three kinds of tumors. Thus (11)C-PD153035 may be used as a positron emission tomography tracer to yield useful information about tumors, particularly for lung cancer with different EGFR expression levels.
authors.affiliation: Medical School of Shandong University, Wenhua West Road 44, Jinan, Shandong 250012, China.
authors.forename: Hui
authors.initials: H
authors.lastname: Wang
authors.forename: Jinming
authors.initials: J
authors.lastname: Yu
authors.forename: Guoren
authors.initials: G
authors.lastname: Yang
authors.forename: Xianrang
authors.initials: X
authors.lastname: Song
authors.forename: Xiaorong
authors.initials: X
authors.lastname: Sun
authors.forename: Shuqiang
authors.initials: S
authors.lastname: Zhao
authors.forename: Dianbin
authors.initials: D
authors.lastname: Mu
mesh_terms: D000818:Animals; D014408:Biomarkers, Tumor / Q000378:metabolism; D002250:Carbon Radioisotopes / Q000378:metabolism*; D045744:Cell Line, Tumor; D066246:ErbB Receptors / Q000096:biosynthesis* / Q000235:genetics* / Q000378:metabolism; D005260:Female; D006801:Humans; D008175:Lung Neoplasms / Q000378:metabolism; D008325:Mammary Neoplasms, Experimental / Q000378:metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D009928:Organ Specificity; D049268:Positron-Emission Tomography; D011799:Quinazolines / Q000378:metabolism*
chemical_list: D014408:Biomarkers, Tumor; D002250:Carbon Radioisotopes; D011799:Quinazolines; D066246:ErbB Receptors; C088860:4-((3-bromophenyl)amino)-6,7-dimethoxyquinazoline