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 language||English (US)|
|Number of pages||5|
|State||Published - 1990|
ASJC Scopus subject areas
- Organic Chemistry
- Clinical Biochemistry
- Biochemistry, Genetics and Molecular Biology(all)