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. 2020 Nov 23;12(4):1458–1468. doi: 10.1039/d0sc05191h

Comparison between the two-step approaches via electrophilic or nucleophilic pathway and the arylboronic acid method for the 125I-iodination and 211At-astatination of the 9E7.4 mAb.

Method RCYs (%) Activity yieldc (MBq) Specific activityc (MBq mg−1) Duration time (min)
125I 211At 125I 211At 125I 211At
Two-step electrophilica 20–30 5.5 24.4 200 ± 10
Two-step nucleophilicb 43 53–57 12.9 13.2 57.3 58.7 140 ± 10
This work 80 56–68 24 16.1 66.7 119 90 ± 10
a

[211At]SAB prepared from the tin precursor with N-chlorosuccinimide as oxidizing agent before the conjugation to the mAb (n = 2).

b

[125I]SIB or [211At]SAB prepared from the aryliodonium salt with sodium sulfite as reducing agent before conjugation to the mAb (n = 5).

c

Starting with 30 MBq.