PSMA inhibitor | IC50 | %Internalization compared to the referenceb | log D |
---|---|---|---|
natLu/[177Lu]Lu-1 | 2.8 ± 0.5 nM | 1 h: 177 ± 15 | −3.78 ± 0.01 |
natGa-2 | >  3 μM (n = 2) | n.d. | n.d. |
natGa-3 | 21.3 ± 1.7 nM | n.d. | n.d. |
natLu/[177Lu]Lu-3 | 7.1 ± 0.7 nM | 1 h: 67.8 ± 0.5 | − 3.40 ± 0.45 |
natGa-4 | >  1 μM (n = 2) | n.d. | n.d. |
natLu/[177Lu]Lu-5 | 26 ± 16 μM | 0.5 h: 0.00 ± 0.00 1 h: 0.00 ± 0.00 2 h: 0.17 ± 0.32 4 h: 0.01 ± 0.05 | −2.89 ± 0.18 |
natLu/[177Lu]Lu-6 | 2.5 ± 1.2 μM | 0.5 h: 0.00 ± 0.00 1 h: 0.00 ± 0.10 2 h: 0.03 ± 0.03 4 h: 0.01 ± 0.06 | −2.52 ± 0.22 |
natLu/[177Lu]Lu-7 | 6.3 ± 3.6 μM | 0.5 h: 0.00 ± 0.00 1 h: 0.00 ± 0.00 2 h: 0.00 ± 0.00 4 h: 0.00 ± 0.00 | −2.37 ± 0.22 |
natLu-8 | >  2 μM (n = 2) | n.d. | n.d. |
natLu-9 | >  440 nM (n = 2) | n.d. | n.d. |
natLu/[177Lu]Lu-10 | 138 ± 53 nM | 1 h: 1.2 ± 0.4 | − 2.83 ± 0.08 |
natLu/[177Lu]Lu-11 | 16.4 ± 3.8 nM | 1 h: 9.9 ± 3.2 | − 2.91 ± 0.05 |