用于放射性砹(碘)标记蛋白质的偶联剂SPC的合成及表征

  • 摘要: 以5-溴烟酸为起始物,通过3步主要反应合成了一种适用于蛋白质放射性砹(碘)标记的偶联剂——5-(三正丁基锡)-3-吡啶甲酸 N-琥珀酰亚胺酯(SPC),并用核磁共振(NMR)、质谱(MS)、高效液相色谱(HPLC)等进行了表征。以该试剂为双功能偶联剂,实现了IgG的~(125)I标记,标记率达30%以上。标记产物在体外具有较高的稳定性。

     

    Abstract: N-succinimidyl 5--(tributylstannyl)-3-pyridinecarboxylate (SPC), a useful linker forlabeling proteins with astatine and iodine radioisotopes, is synthesized in three steps with 5-bromonicotinic acid as a starting material, and is characterized by nuclear magnetic resonance(NMR), mass spectrometer(MS) and high performance liquid chromatography (HPLC). Withthis bi-functional ester, ~(125)I labeled human IgG is performed in labeling yield of approximately30%. Also, the in vitro stability of the prepared ~(125)I-IgG is evaluated.

     

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