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目的研究(153)Sm通过二乙三胺五乙酸(DTPA)环酐(cDTPAa)为双功能络合剂标记抗CEA单抗的方法。方法确定cDTPAa与抗体偶联的最佳条件,并测定偶联物的免疫活性及在体外的稳定性。结果(153)Sm标记抗CEA单抗的方法简便、快速,且抗体与cDTPAa偶联后其免疫活性无明显丧失。在抗体浓度为20mg/ml时,最佳偶联条件为:抗CEA单抗与cDTPAa的摩尔比为1:20,偶联反应中pH为7~8。在最佳偶联条件下,用高比活度的(153)Sm(22.2SGBq/ml),CEAMcAb-DTPA的标记率可达60%。结论通过DTPA环酐法将(153)Sm标记到单抗上所制备的放射免疫偶联物可作为一种有希望的放射免疫治疗剂。
AIM To investigate (153) a method for labeling anti-CEA mAb with Sm via bis-functional complexing agent with diethylenetriaminepentaacetic acid (DTPA) cyclic anhydride (cDTPAa). Methods The optimal conditions for conjugation of cDTPAa to the antibody were determined and the conjugate was tested for its immunocompetence and in vitro stability. Results (153) Sm-labeled anti-CEA monoclonal antibody method is simple and rapid, and the antibody and cDTPAa conjugate without significant loss of its immunocompetence. When the antibody concentration was 20mg / ml, the optimal coupling conditions were as follows: the molar ratio of anti-CEA McAb to cDTPAa was 1:20, and the coupling reaction pH was 7-8. With the best specific coupling conditions, CEAMcAb-DTPA could be labeled at 60% with a high specific activity of (153) Sm (22.2SGBq / ml). CONCLUSION Radioimmunoconjugates prepared by labeling (153) Sm with a DTPA cyclic anhydride method can be used as a promising radioimmunotherapy.