Optimization of preparation of Rh-105 labeled (B72.3) MOAB using an amine oxime ligand and comparison of its biodistribution with I-131 labeled B72.3 MOAB
- Bhabha Atomic Research Center, Bombay (India)
- Univ. of Missouri, Columbia, MO (United States); and others
Propyleneamineoxime ligands with the four N donor atoms form stable complexes with Rh(III). The p-aminobenzylpropyleneamineoxime ligand (L) was made to act as a bifunctional chelating agent to label proteins with Rh-105. This study encompasses the optimization of formation of the Rh-105 complex of L, its purification, activation with thiophosgene, conjugation the B72.3 MOAB, purification by gel filtration, determination of its stability in physiological buffers and in human serum and comparison of the biodistribution Rh-105 labeled antibody with I-131 labeled antibody in normal healthy mice. Rh-105 was complexed with the ligand L by refluxing at pH 5-6 for 45 min. CuCl, was added to form a charged complex and the neutral activated Rh-105 complex extracted into chloroform. Following evaporation of CHC1{sub 3}, the complex was dissolved in 20 {mu}1 of DMF and reconstituted with 0.5 ml of saline. This was then reacted with the B72.3 MOAB in 0.05 M bicarbonate buffer at pH 9 and incubated for 3 h at 37{degrees}C. The complexation yields were generally 95% and the conjugation yields {approximately}60%. The Rh-105 conjugate was stable at room temperature in phosphate buffer saline (pH 7.4), bicarbonate buffer saline (pH 8.5) and human serum at 37{degrees}C for 4 days. >95% of the conjugate remained immunoreactive using mucin-bound to sepharose as the antigen. I-131 labeled antibody was prepared by using iodogen as the oxidizing agent. The two labeled antibodies were co-injected into healthy mice and the biodistribution studied at different time intervals. The biodistribution studies show good correlation between I-131 and Rh-105 labeled B72.3 MOAB preparations over 20 h demonstrating good in vivo stability. This ligand may be useful as a bifunctional chelating agent for Rh-105 labeled antibody.
- DOE Contract Number:
- FG02-86ER60400
- OSTI ID:
- 198099
- Report Number(s):
- CONF-940605-; ISSN 0161-5505; TRN: 95:007029-0251
- Journal Information:
- Journal of Nuclear Medicine, Vol. 35, Issue Suppl.5; Conference: 41. annual meeting of the Society of Nuclear Medicine, Orlando, FL (United States), 5-8 Jun 1994; Other Information: PBD: May 1994
- Country of Publication:
- United States
- Language:
- English
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