Open AccessAssessment of 11 C‐labeled‐4‐ N ‐(3‐bromoanilino)‐6, 7‐dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression
Author(s) -
Wang Hui,
Yu Jinming,
Yang Guoren,
Song Xianrang,
Sun Xiaorong,
Zhao Shuqiang,
Mu Dianbin
Publication year - 2007
Publication title -
cancer science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.035
H-Index - 141
eISSN - 1349-7006
pISSN - 1347-9032
DOI - 10.1111/j.1349-7006.2007.00562.x
Subject(s) - biodistribution , epidermal growth factor receptor , positron emission tomography , in vivo , ex vivo , in vitro , epidermal growth factor , receptor expression , chemistry , cancer research , pathology , nuclear medicine , microbiology and biotechnology , receptor , biology , medicine , biochemistry
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. ( Cancer Sci 2007; 98: 1413–1416)