@article{oai:repo.qst.go.jp:00045755,
 author = {Sogawa, Chizuru and Tsuji, Atsushi and Sudou, Hitomi and Sugyou, Aya and Yoshida, Chisato and Odaka, Kenichi and Uehara, Tomoya and Arano, Yasushi and Koizumi, Mitsuru and Saga, Tsuneo and 曽川 千鶴 and 辻 厚至 and 須藤 仁美 and 須尭 綾 and 吉田 千里 and 小高 謙一 and 上原 知也 and 荒野 泰 and 小泉 満 and 佐賀 恒夫},
 issue = {2},
 journal = {Nuclear Medicine and Biology},
 month = {Feb},
 note = {Introduction: Gastrointestinal stromal tumor (GIST) is the most common mesenchymal tumor arising from the gastrointestinal tract and highly expresses mutated c-kit. 
We aimed to develop a specific and sensitive method for detecting GISTs using radiolabeled anti-c-kit monoclonal antibody.
Methods: A mutated c-kit-expressing cell clone was established by transfecting an expressing vector of mutated c-kit gene into HEK293 human embryonic kidney cells. The tumors were developed by inoculating c-kit-expressing cells into nude mice. 125I- and 111In-labeled anti-c-kit antibodies (12A8 and 41A11) were evaluated in vitro by cell binding, competitive inhibition and cellular internalization assays, and in vivo by biodistribution and imaging studies in tumor-bearing mice.
Results: Both 125I- and 111In-labeled antibodies showed specific binding with c-kit-expressing cells with high affinity (dissociation constants
= 2.2-7.1x109 M-1). Internalization assay showed that 125I-labeled antibodies were rapidly internalized and dehalogenated, with the release of 125I from the cells, resulting in reduction of cell-associated radioactivity with time. In contrast, 111In-labeled antibody was internalized but did not result in the reduced radioactivity associated with tumor cells. Reflecting this phenomenon, the in vivo tumor uptake of 125I-labeled antibody was low on Day 1, further decreasing with time, while tumor uptake of 111In-labeled antibody was high on Day 1, further increasing with time. 
The xenografted tumor was clearly visualized by scintigraphy after injection of 111In-labeled antibody.
Conclusion: The anti-c-kit monoclonal antibody labeled with a metal radionuclide would be promising for c-kit-targeted imaging of GISTs.},
 pages = {179--187},
 title = {C-kit-targeted imaging of gastrointestinal stromal tumor using radiolabeled anti-c-kit monoclonal antibody in a mouse tumor model},
 volume = {37},
 year = {2010}
}