m-[125I]碘苯胺:一种有用的生物素放射性标记试剂

Leslie A. Khawli , Amin I. Kassis
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引用次数: 4

摘要

以生物素和m-[125I]碘苯胺为原料,经混合酸酐反应合成生物素-m-[125I]碘苯胺(BIA)。以六丁基二丁与间溴苯胺为原料,钯催化制得m-[125I]碘苯胺。放射性碘化BIA衍生物的特征是在生物素分子上有稳定的酰胺和/或完整的脲基;因此,它可能是将放射性核素靶向于先前定位于肿瘤上的亲和蛋白结合抗体的有用载体。
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m-[125I]iodoaniline: a useful reagent for radiolabeling biotin

Biotinyl-m-[125I]iodoanilide (BIA) was synthesized by coupling biotin to m-[125I]iodoaniline via a mixed anhydride reaction. m-[125I]Iodoaniline was produced from the tin precursor, which was prepared using a palladium catalyzed reaction of hexabutylditin with m-bromoaniline. The radioiodinated BIA derivative is characterized by a stable amide and/or intact ureido group on the biotin molecule; it may thus be a useful carrier for targeting radionuclides to avidin-conjugated antibodies previously localized on tumors.

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