Conjugation of phenyl isothiocyanate derivatives of carborane to antitumor antibody and in vivo localization of conjugates in nude mice

摘要: A systematic study of the conjugation 1-(p-isothiocyanatophenyl)-1,2-dicarba-closo-[2-3H]dodeca borane(12), 3H-1, and 7-(p-isothiocyanatophenyl)dodecahydro-7,8-dicarba-nido -[8-3H] undecaborate(1-)ion, 3H-2, to murine monoclonal anti-CSAp antibody, Mu-9, was carried out compare charged uncharged boron cages in their effect upon antibody loading. Approximately one neutral cage four anionic were successfully linked two separate conjugates which subsequently radioiodinated evaluated vivo. No significant loss or its immunoreactivity observed either case. In nude mice bearing GW-39 tumor xenografts conjugate containing carborane derivative showed a reduced uptake although tumor:non-tumor ratio similar that native antibody. The 2 radiolabeled with 125I followed by attempts purify product 4 model goat IgG protein. This exploratory undertaken as prelude linking new reagents, contain multiple cages, antitumor antibodies. latter are required maximize loading for purpose neutron-capture therapy.