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EJNMMI Research

Table 2 Affinity toward SST2 and SST5 of all four natGa-DOTA-conjugates compared to reference somatostatin analogs

From: A new 68Ga-labeled somatostatin analog containing two iodo-amino acids for dual somatostatin receptor subtype 2 and 5 targeting

Compounds

SST2

SST5

IC50, nM (95% CI)

IC50, nM (95% CI)

Somatostatin-14* (1)

0.11 (0.08–0.15)

0.35 (0.22–0.55)

natGa-DOTA-ST8950

0.32 (0.20–0.50)

1.9 (1.1–3.1)

natGa-DOTA-ST8951

7.5 (5.2–11)

24 (14–43)

natGa-DOTA-TATE

0.15 (0.11–0.19)

69 (28–168)

natGa-DOTA-NOC

0.70 (0.50–0.96)

3.4 (1.8–6.2)

ST8950 (1)

0.28 (0.19–0.42)

0.77 (0.48–1.2)

Octreotide (1)**

0.24 (0.12–0.48)

17 (12–24)

Pasireotide (1)**

3.1 (2.0–4.9)

0.20 (0.11–0.35)

  1. Experiments were performed in 3 to 5 separate sessions in duplicate
  2. *Somatostatin-14 is the natural ligand and was used as control
  3. **Octreotide and pasireotide were used for comparison, additionally to natGa-DOTA-TATE and natGa-DOTA-NOC
  4. (1)From [25]
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