|
Ligand
|
IC50 [nM]
|
Internalization [% of reference]
|
Lipophilicity [log POW]
|
|---|
|
In-PSMA-I&T
|
7.5 ± 1.5
|
104 ± 7
|
−4.5
|
|
Ga-PSMA-I&T
|
9.4 ± 2.9
|
59 ± 2
|
−4.3
|
|
Lu-PSMA-I&T
|
7.9 ± 2.4
|
76 ± 2
|
−4.1
|
- PSMA affinities were determined in a competitive binding assay using LNCaP prostate cancer cells and (125I-BA)KuE as radioligand [2]. Data represent means ± SD of n ≥ 3 separate determinations
- PSMA-specific ligand internalization was determined by incubation of LNCaP cells (37 °C, 60 min) with the respective radioligands (0.2 nM) in the absence (total internalization) and presence (non-specific internalization) of 10 μM PMPA. Data were corrected for non-specific internalization and normalized to the specific internalization observed for the reference compound (125I-BA)KuE in a parallel experiment [2]. Data are means ± SD (n = 3)
- Lipophilicities (from n-octanol/PBS partition coefficients POW) were determined using a shake-flask method; values are means from n = 6 determinations
