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EJNMMI Research

Table 1 PSMA affinities (IC 50 ) of the compounds investigated

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

Ligand

IC50[nM]

HBED-CC-Ahx-KuE

 

5.7 ± 0.5

[natGa]HBED-CC-Ahx-KuE

 

6.1 ± 0.8

DOTA-FFK(Sub-KuE)

(10)

13.1 ± 2.3

[natGa]DOTA-FFK(Sub-KuE)

(natGa-10)

29.5 ± 6.6

[natLu]DOTA-FFK(Sub-KuE)

(natLu-10)

54.7 ± 6.1

DOTAGA-FFK(Sub-KuE)

(11)

10.2 ± 1.5

[natGa]DOTAGA-FFK(Sub-KuE)

(natGa-11)

12.1 ± 3.9

[natLu]DOTAGA-FFK(Sub-KuE)

(natLu-11)

15.1 ± 1.5

DOTAGA-ffk(Sub-KuE)

(12)

13.9 ± 0.4

[natGa]DOTAGA-ffk(Sub-KuE)

(natGa-12)

15.9 ± 0.5

[natLu]DOTAGA-ffk(Sub-KuE)

(natLu-12)

13.1 ± 2.2

  1. Binding assays were performed using LNCaP cells (150,000/well) and ([125I]I-BA)KuE (c = 0.2 nM) as the radioligand. Cells were incubated in HBSS (1% BSA) at 4°C for 1h. Data are expressed as mean ± SD (n = 3).
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