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EJNMMI Radiopharmacy and Chemistry

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

From: Targeting fibroblast activation protein (FAP): next generation PET radiotracers using squaramide coupled bifunctional DOTA and DATA5m chelators

 

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

  1. aDetermined under the conditions of this study. b data from Jansen et al. (Jansen et al. 2014a)
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