Cell Binding and Internalization of Dye Conjugates in Comparison to PSMA-11 (25,27)
| 68Ga-labeled compounds | IC50 (nM) | |||
| Compound | Specifically cell surface–bound (%IA) | Specifically internalized (%IA) | Metal-free ligands | 69/71Ga-labeled compounds |
| PSMA-11 | 18.31 ± 0.71 | 3.54 ± 0.28 | 19.19 ± 7.42 | 12.1 ± 2.1 |
| Glu-urea-Lys-HBED-CC-FITC | 1.28 ± 0.20 | 4.89 ± 0.93 | 11.14 ± 1.16 | 10.52 ± 1.47 |
| Glu-urea-Lys-HBED-CC-AlexaFluor488 | 5.22 ± 0.25 | 14.96 ± 0.81 | 13.32 ± 0.83 | 25.59 ± 3.93 |
| Glu-urea-Lys-HBED-CC-IRDye800CW | 13.62 ± 4.79 | 18.70 ± 7.03 | 24.54 ± 5.70 | 35.54 ± 2.94 |
| Glu-urea-Lys-HBED-CC-DyLight800 | 10.50 ± 3.64 | 13.88 ± 7.04 | 21.41 ± 1.90 | 21.23 ± 4.26 |
%IA = percentage of applied radioactivity bound to 105 cells (specific cell uptake was determined by blockage using 500 μM 2-(phosphonomethyl)-pentanedioic acid); FITC = fluorescein isothiocyanate.
Data are mean ± SD (n = 3).