In this study, the feasibility of constructing radioimmunoconjugates by using the novel therapeutic candidate alpha-emitter, 227 Th, was evaluated. By use of the bifunctional chelator, p-SCN-benzyl-DOTA, 227 Th was conjugated to the two monoclonal antibodies, rituximab and trastuzumab. Their stability in 80% fetal bovine serum at 37°C was measured. The immunoreactive fractions were determined by using CD20and HER/2-positive cells, respectively. The overall labeling yield spanned from 6% to 17%. The radioimmunoconjugates demonstrated a relevant stability in serum and showed appropriate antigen-binding abilities.
An alternative one-step method for determination of parameters describing binding of antibodies to antigens on cells has been developed. The method gives reliable estimates of affinity and number of antigens and in addition gives information on the kinetics of binding.
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