Table 2.
Comparison between arylstannane chemistry (method A & B, see details in ESI) from the literature and our aryliodonium salts approach for the astatination of the 9E7.4 antibody.
| [211At]SAB RCY (%)d | Conjugation yield (%)e | Overall decay corrected RCY (%) | Procedure duration (min) | |
|---|---|---|---|---|
| Method Aa | 33–58f | 51–61 | 20–30 | 200 ± 10 |
| Method Bb | 75–93 | 27–30 | 24–29 | 120 ± 10 |
| This workc | 77–84 | 54–60 | 53–57 | 140 ± 10 |
SAB produced from the tin precursor with N-chlorosuccinimide as oxidizing agent and purified by HPLC before conjugation (n = 2).
SAB produced from the tin precursor with N-iodosuccinimide as oxidizing agent and conjugated crude without purification (n = 3).
SAB produced from aryliodonium 4a and purified on a silica Sep-Pak Vac 3cc (500 mg) cartridge before conjugation (n = 5).
Decay corrected RCYs of purified [211At]SAB.
Conjugation yields are given after purification by gel filtration. Such purification leads typically to 20–25% loss of radiolabeled antibody on the purification column.
Crude RCY was typically 70–90%; major loss due to HPLC purification.