title: Development of 3-iodophenylisothiocyanate for radioiodination of monoclonal antibodies.
abstract: A new radioiodination reagent, 3-iodophenylisothiocyanate (3-IPI) has been developed for coupling to monoclonal antibodies. The starting material, 3-tri-n-butylstannylphenylisothiocyanate was prepared via a reaction of hexabutylditin with 3-bromoaniline, followed by treatment with thiophosgene with an overall yield of 72%. The radioiodination of this tin precursor with Na[125I]I/iodogen in chloroform gave 3-[125I]IPI in 23-55% radiochemical yield and 81-99.6% radiochemical purity. Purification of the impure product by high pressure liquid chromatography increased the radiochemical purity of the product up to 99%. These results suggest that 3-IPI may be a useful ligand for radioiodination and coupling to a variety of monoclonal antibodies.
authors.affiliation: Department of Radiation Oncology, University of Alabama, Birmingham 35233-6832.
authors.forename: S
authors.initials: S
authors.lastname: Ram
authors.forename: D J
authors.initials: DJ
authors.lastname: Buchsbaum
mesh_terms: D000911:Antibodies, Monoclonal; D007457:Iodine Radioisotopes; D017879:Isothiocyanates; D007553:Isotope Labeling / Q000379:methods*; D013861:Thiocyanates / Q000138:chemical synthesis*
chemical_list: D000911:Antibodies, Monoclonal; D007457:Iodine Radioisotopes; D017879:Isothiocyanates; D013861:Thiocyanates; C078466:3-iodophenylisothiocyanate