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Potentially nonadentate (N 5 O 4 ) bifunctional chelator p-SCN-Bn-H 4 neunpa and its immunoconjugate H 4 neunpa-trastuzumab for 111 In radiolabeling are synthesized. The ability of p-SCN-Bn-H 4 neunpa and H 4 neunpa-trastuzumab to quantitatively radiolabel 111 InCl 3 at an ambient temperature within 15 or 30 min, respectively, is presented. Thermodynamic stability determination with In 3+ , Bi 3+ , and La 3+ resulted in high conditional stability constant (pM) values. In vitro human serum stability assays have demonstrated both 111 In complexes to have high stability over 5 days. Mouse biodistribution of [ 111 In][In(p-NO 2 -Bn-neunpa)] - , compared to that of [ 111 In][In(p-NH 2 -Bn-CHX-A″-diethylenetriamine pentaacetic acid (DTPA))] 2- , at 1, 4, and 24 h shows fast clearance of both complexes from the mice within 24 h. In a second mouse biodistribution study, the immunoconjugates 111 In-neunpa-trastuzumab and 111 In-CHX-A″-DTPA-trastuzumab demonstrate a similar distribution profile but with slightly lower tumor uptake of 111 In-neunpa-trastuzumab compared to that of 111 In-CHX-A″-DTPA-trastuzumab. These results were also confirmed by immuno-single photon emission computed tomography (immuno-SPECT) imaging in vivo. These initial investigations reveal the acyclic bifunctional chelator p-SCN-Bn-H 4 neunpa to be a promising chelator for 111 In (and other radiometals) with high in vitro stability and also show H 4 neunpa-trastuzumab to be an excellen 111 In chelator with promising biodistribution in mice.

bioconjugate chemistry

p-NO2–Bn–H4neunpa and H4neunpa–Trastuzumab: Bifunctional Chelator for Radiometalpharmaceuticals and 111In Immuno-Single Photon Emission Computed Tomography Imaging