Table 1.
IC50-values of DOTA.SA.FAPi, the natGa and natLu-complexes and DATA5m.SA.FAPi and the natGa-complex with regard to FAP and PREP. Selectivity index gives the ratio FAP to PREP
| IC50 FAP (nM) | IC50 PREP (μM) | Selectivity index (IC50 (FAP/PREP)) | |
|---|---|---|---|
| DOTA.SA.FAPi – uncomplexed | 0.9 ± 0.1 | 5.4 ± 0.3 | 6000 |
| DOTA.SA.FAPi - natGa | 1.4 ± 0.2 | 8.7 ± 0.9 | 6214 |
| DOTA.SA.FAPi – natLu | 0.8 ± 0.2 | 2.5 ± 0.4 | 3125 |
| DATA5m.SA.FAPi – uncomplexed | 0.8 ± 0.2 | 1.7 ± 0.1 | 2113 |
| DATA5m.SA.FAPi – natGa | 0.7 ± 0.1 | 4.7 ± 0.3 | 6714 |
| FAP-inhibitor UAMC1110 | 0.43 ± 0.07a | 1.8 ± 0.2b | 4186 |
aDetermined under the conditions of this study. b data from Jansen et al. (Jansen et al. 2014a)