Preparation and chemical characterization of radioiodinated bleomycin

J. Meyers, Kenneth Krohn, G. DeNardo

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Abstract

None of the radionuclides with which bleomycin has been labeled have chemical and nuclear properties that are entirely satisfactory for in vivo tumor localization. Bleomycin has been radioiodinated by the iodine monochloride, chloramine T, and lactoperoxidase methods. Iodine monochloride proved to be the preferred method and conditions were developed whereby 80% of radioiodide was covalently bound to bleomycin. Bleomycin (140 μg) was added to 200 μl of saline/citrate buffer (pH 7.0) followed by radioiodide and iodine monochloride. This reaction mixture was incubated for 1 hr and purified by Sephadex G 10 chromatography. The iodine monochloride reaction product underwent hydrolytic deiodination in vitro at a rate of about 1.2%/day (0.15 M NaCl, 37°C). Bleomycin A and B components were radioiodinated with equal efficiency on a mole fraction basis.

Original languageEnglish (US)
Pages (from-to)835-838
Number of pages4
JournalJournal of Nuclear Medicine
Volume16
Issue number9
Publication statusPublished - 1975
Externally publishedYes

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ASJC Scopus subject areas

  • Radiological and Ultrasound Technology

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