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Table 2 Internalization of radiometalated ligands in percentage of external reference ([125I]I-BA)KuE

From: Synthesis and preclinical evaluation of DOTAGA-conjugated PSMA ligands for functional imaging and endoradiotherapy of prostate cancer

Ligand Internalization(1 h)in%of([125I]I-BA)KuE
[68Ga]HBED-CC-Ahx-KuE   91.1 ± 1.7
[68Ga]DOTA-FFK(Sub-KuE) (68Ga-10) 14.6 ± 0.8
[177Lu]DOTA-FFK(Sub-KuE) (177Lu-10) 19.3 ± 0.9
[68Ga]DOTAGA-FFK(Sub-KuE) (68Ga-11) 28.4 ± 0.7
[177Lu]DOTAGA-FFK(Sub-KuE) (177Lu-11) 36.1 ± 1.1
[68Ga]DOTAGA-ffk(Sub-KuE) (68Ga-12) 42.5 ± 1.7
[177Lu]DOTAGA-ffk(Sub-KuE) (177Lu-12) 44.4 ± 1.8
  1. Data is corrected for unspecific binding, c = 0.2 nM for 68Ga, c = 0.5 nM for 177Lu compounds, 37°C, 1 h, 125,000 cells/well, PLL-coated plates.