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

Nucl Med Biol. 2001 Jan;28(1):33-9. doi: 10.1016/s0969-8051(00)00171-2.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

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

Substances

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