Linder K E, Wen M D, Nowotnik D P, Ramalingam K, Sharkey R M, Yost F, Narra R K, Nunn A D, Eckelman W C
Bristol-Myers Squibb Pharmaceutical Research Institute, New Brunswick, New Jersey 08903.
Bioconjug Chem. 1991 Nov-Dec;2(6):407-14. doi: 10.1021/bc00012a005.
BATO (boronic acid adduct of technetium dioximes) complexes, TcCl(dioxime)3BR, were prepared in which the boron substituent (R) was the protein-reactive 2-carboxy-4-phenyl isothiocyanate (CPITC). The 99Tc complexes, where the dioxime was either dimethylglyoxime (DMG) or cyclohexanedione dioxime (CDO), were prepared and characterized. The 99mTc complex TcCl(DMG)3CPITC was prepared from a freeze-dried kit and used to label B72.3 (anti-TAG.72) and NP-4 (anti-CEA) whole antibodies, and the NP-4 F(ab')2 fragment. SDS-PAGE electrophoresis indicated that the labeling reagent was strongly bound to antibody. The labeled antibodies displayed high binding to affinity columns and good tumor uptake in GW39 tumor-bearing mice.
制备了BATO（二肟硼酸锝加合物）配合物TcCl(dioxime)3BR，其中硼取代基（R）为蛋白质反应性的2-羧基-4-苯基异硫氰酸酯（CPITC）。制备并表征了以二肟为二甲基乙二肟（DMG）或环己二酮二肟（CDO）的99Tc配合物。99mTc配合物TcCl(DMG)3CPITC由冻干试剂盒制备，并用于标记B72.3（抗TAG.72）和NP-4（抗CEA）全抗体以及NP-4 F(ab')2片段。SDS-PAGE电泳表明标记试剂与抗体紧密结合。标记抗体在GW39荷瘤小鼠中显示出对亲和柱的高结合力和良好的肿瘤摄取。
