用于单克隆抗体放射性碘化的3-碘苯基异硫氰酸酯的研发。

Development of 3-iodophenylisothiocyanate for radioiodination of monoclonal antibodies.

作者信息

Ram S, Buchsbaum D J

机构信息

Department of Radiation Oncology, University of Alabama, Birmingham 35233-6832.

出版信息

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

DOI:10.1016/0883-2889(92)90013-5

PMID:1333460

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.

摘要

一种用于与单克隆抗体偶联的新型放射性碘化试剂——3-碘苯基异硫氰酸酯（3-IPI）已被开发出来。起始原料3-三正丁基锡基苯基异硫氰酸酯是通过六丁基二锡与3-溴苯胺反应制备的，随后用硫光气处理，总产率为72%。该锡前体在氯仿中用Na[¹²⁵I]I/碘珠进行放射性碘化反应，得到放射性化学产率为23 - 55%、放射性化学纯度为81 - 99.6%的3-[¹²⁵I]IPI。通过高压液相色谱法对不纯产物进行纯化，可将产物的放射性化学纯度提高到99%。这些结果表明，3-IPI可能是一种用于放射性碘化及与多种单克隆抗体偶联的有用配体。