High-efficiency astatination of antibodies using N-iodosuccinimide as the oxidising agent in labelling of N-succinimidyl 3-(trimethylstannyl)benzoate.

Abstract

Monoclonal antibodies C215, reactive with colorectal carcinomas, and MOv18, reactive with most of the ovarian carcinomas, were radiohalogenated with [211At]astatine. The radiohalogen was conjugate coupled to antibodies via the intermediate labelling reagent N-succinimidyl-3-(trimethylstannyl)benzoate (m-MeATE) in a two-step, single-pot reaction. Optimisation of the labelling of the reagent was achieved using N-iodosuccinimide, NIS, as the oxidising agent. The yields ranged from 69-95% in the labelling of 0.1-1.0 nmole of the m-MeATE precursor. Subsequent conjugation to antibodies resulted in yields of 58+/-7%. In vitro binding to tumour cells showed that the immunoreactivity of both antibodies was retained after astatine labelling.

• Authors: S Lindegren, H Andersson, T Bäck, L Jacobsson, B Karlsson, G Skarnemark
• Journal: Nuclear medicine and biology (Nucl Med Biol) Vol. 28 Issue 1 Pg. 33-9 (Jan 2001) ISSN: 0969-8051 [Print] United States
• PMID: 11182562 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antibodies, Monoclonal
• Benzoates
• Succinimides
• Trimethyltin Compounds
• N-succinimidyl 3-(trimethylstannyl)benzoate
• N-iodosuccinimide
• Astatine

Topics

• Antibodies, Monoclonal (immunology, metabolism)
• Astatine (immunology, metabolism)
• Benzoates (immunology)
• Colorectal Neoplasms (diagnostic imaging, immunology, metabolism)
• Humans
• Radionuclide Imaging
• Succinimides (chemistry)
• Trimethyltin Compounds (immunology)
• Tumor Cells, Cultured (diagnostic imaging, immunology, metabolism)