Simplified method for conjugating macrocyclic bifunctional chelating agents to antibodies via 2-iminothiolane

Michael J. McCall, Habibe Diril, Claude F. Meares

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101 Scopus citations


A one-step method for conjugating macrocyclic chelators to antibodies using the protein modification reagent 2-iminothiolane controls aggregation, maintains immunoreactivity, and produces consistent chelate/antibody ratios. Conjugation conditions have been investigated with the macrocyclic chelates 6-[p-(bromoacetamido)benzyl]-1,4,8,11-tetraazacyclotetradecane-N,N′, N″,N‴-tetraacetic acid and 2-[p-(bromoacetamido)benzyl]-1,4,7,10-tetraazacydododecane-N,N′,N″, N′-tetraacetic acid, with three different monoclonal antibodies. The bifunctional chelating agents are prepared by bromoacetylation of their amine precursors using a two-phase H2O/CHCl3 system, which improves product purity.

Original languageEnglish (US)
Pages (from-to)222-226
Number of pages5
JournalBioconjugate Chemistry
Issue number3
StatePublished - 1990


ASJC Scopus subject areas

  • Chemistry(all)
  • Organic Chemistry
  • Clinical Biochemistry
  • Biochemistry, Genetics and Molecular Biology(all)
  • Biochemistry

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