Analytic Data and In Vitro Properties of [61Cu]Cu-DOTAGA-PSMA-I&T and [61Cu]Cu-NODAGA-PSMA-I&T
| Radioligand | RCP | tR (min) | logDpH7.4 | IC50 (nM)* | Internalized fraction (%) | Surface-bound fraction (%) |
|---|---|---|---|---|---|---|
| [61Cu]Cu-DOTAGA-PSMA-I&T | 97.4 ± 2.3 | 7.2 ± 0.2 | −2.69 ± 0.44 | 11.2 ± 2.3 | 13.3 ± 0.5 | 13.4 ± 0.8 |
| [61Cu]Cu-NODAGA-PSMA-I&T | 98.2 ± 1.9 | 7.0 ± 0.3 | −2.95 ± 0.08 | 9.3 ± 1.8 | 11.7 ± 1.6 | 10.8 ± 1.8 |
↵* Determined using natCu-DOTAGA-PSMA-I&T and natCu-NODAGA-PSMA-I&T complexes.
RCP = radiochemical purity; tR = retention time.
RCP and tR refer to radio–high-performance liquid chromatography analysis. Lipophilicity (logD) was determined in 1:1 mixture of octanol–to–phosphate-buffered saline at pH 7.4. IC50 values were determined in competition assays on LNCaP cells using ((S)-1-carboxy-5-(4-(-125I-iodo-benzamido)pentyl)carbamoyl)-l-glutamic acid at concentration of 0.2 nM. Internalized and surface-bound fractions refer to percentage of applied activity after 1 h of incubation of LNCaP cells with radiotracer at 37°C. All results are expressed as mean ± SD.