Development of 3-iodophenylisothiocyanate for radioiodination of monoclonal antibodies

Int J Rad Appl Instrum A. 1992 Nov;43(11):1387-91. doi: 10.1016/0883-2889(92)90013-5.

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.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Antibodies, Monoclonal*
  • Iodine Radioisotopes
  • Isothiocyanates*
  • Isotope Labeling / methods*
  • Thiocyanates / chemical synthesis*

Substances

  • Antibodies, Monoclonal
  • Iodine Radioisotopes
  • Isothiocyanates
  • Thiocyanates
  • 3-iodophenylisothiocyanate