Chanachai W, Shani J, Wolf W, Harwig J F, Nakamura R M
Int J Nucl Med Biol. 1985;12(4):289-93. doi: 10.1016/0047-0740(85)90182-2.
A systematic analysis of various factors involved in the CDI-mediated coupling of DTPA to IgG have been carried out, in order to optimize the labeling yield of a monoclonal antibody labeled to high specific activity. Various CDI-to-DTPA ratios were tested, followed by a range of DTPA (activated) to IgG ratios. Specific activities as high as 600 Ci/mmol could be obtained following labeling with 113mIn, when an IgG : DTPA : CDI ratio of 0.01 : 1:20 was used. Other aspects, such as the volume of each of the reactants, the pH and the reaction times, were also standardized to yield a labeled IgG2a (KS1/4) that could be consistently tested for biodistribution and tumor-binding.
为了优化高比活度标记单克隆抗体的标记产率，已对参与CDI介导的DTPA与IgG偶联的各种因素进行了系统分析。测试了各种CDI与DTPA的比例，随后是一系列DTPA（活化的）与IgG的比例。当使用0.01:1:20的IgG:DTPA:CDI比例时，用113mIn标记后可获得高达600 Ci/mmol的比活度。还对其他方面进行了标准化，如每种反应物的体积、pH值和反应时间，以产生可一致用于生物分布和肿瘤结合测试的标记IgG2a（KS1/4）。
