使用N-琥珀酰亚胺基-3-（三甲基锡基）苯甲酸酯作为中间体，在抗体的高比活放射性碘化中使用氯胺-T。

Chloramine-T in high-specific-activity radioiodination of antibodies using N-succinimidyl-3-(trimethylstannyl)benzoate as an intermediate.

作者信息

Lindegren S, Skarnemark G, Jacobsson L, Karlsson B

机构信息

Department of Nuclear Chemistry, Chalmers University of Technology, Sahlgrenska University Hospital, Göteborg, Sweden.

出版信息

Nucl Med Biol. 1998 Oct;25(7):659-65. doi: 10.1016/s0969-8051(98)00033-x.

DOI:10.1016/s0969-8051(98)00033-x

PMID:9804047

Abstract

Monoclonal antibodies C215 and MOv18 have been radiohalogenated, using a single-batch method employing N-succinimidyl-3-(trimethylstannyl)benzoate, m-MeATE. Labelling to the stannyl ester was optimized using chloramine-T as oxidizing agent. The results show that the stannyl ester is effectively labelled with short reaction times giving reproducible yields from 85% to 95%. Subsequent antibody conjugation, 10 to 80 microg MAb, resulted in biologically active, labelled antibodies with overall radiochemical yields of 50% to 80%, with corresponding specific activities of 490-50 kBq(125I)/microg.

摘要

单克隆抗体C215和MOv18已通过使用N-琥珀酰亚胺基-3-（三甲基锡基）苯甲酸酯（m-MeATE）的单批次方法进行了放射性卤化。使用氯胺-T作为氧化剂对锡酯标记进行了优化。结果表明，锡酯在短反应时间内可有效标记，产率可重复，为85%至95%。随后进行抗体偶联，使用10至80微克单克隆抗体，得到具有生物活性的标记抗体，总放射化学产率为50%至80%，相应的比活为490 - 50 kBq(125I)/微克。