Assessment of 11C-labeled-4-N-(3-bromoanilino)-6,7-dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression.
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| 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.
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| Authors | Hui Wang, Jinming Yu, Guoren Yang, Xianrang Song, Xiaorong Sun, Shuqiang Zhao, Dianbin Mu |
| Journal | Cancer science (Cancer Sci) Vol. 98 Issue 9 Pg. 1413-6 (Sep 2007) ISSN: 1347-9032 [Print] England |
| PMID | 17627611 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't) |
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