Influence of catalyst and ligand concentration on radioiodination and astatination RCY of 9E7.4-aBAa.
| Catalyst and ligand concentration (mM) | RCY (%) | |||
|---|---|---|---|---|
| 125I | 211At | |||
| 9E7.4-aBA | 9E7.4 | 9E7.4-aBA | 9E7.4 | |
| 10 | 87 ± 1 | 0.4 | 94 ± 3 | 62 ± 8 |
| 5 | 79 ± 4 | 1.2 | 93 ± 4 | 42 ± 5 |
| 2.5 | 73 ± 2 | — | 96 ± 1 | 32 ± 7 |
| 1.25 | 58 ± 8 | 0.3 | 93 ± 4 | 37 ± 12 |
a
Standard conditions: modified 9E7.4-aBA or unmodified 9E7.4 (32 μM), Cu(OTf)2Pyr4, 1,10-phenanthroline, [125I]NaI or [211At]NaAt (1–5 MBq), 30 min, 23 °C in 0.5 M TRIS buffer/DMF (92.5 : 7.5), n ≥ 3. RCYs are based on the radio-TLC analysis of the crude product.