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Table 4 Stability of 225Ac-Labelled Chelate Complexes in 50-fold excess LaIII at ambient temperature

From: Evaluation of polydentate picolinic acid chelating ligands and an α-melanocyte-stimulating hormone derivative for targeted alpha therapy using ISOL-produced 225Ac

Ligand

% stable

Time point:

1 h

5 h

1 d

2 d

3 d

6 d

7 d

[225Ac(octapa)] (n = 2)

78.9 ± 2.9

42.7 ± 0.3

4.7 ± 1.5

6.1 ± 2.6

NDa

NDa

NDa

[225Ac(CHXoctapa)] (n = 2)

NDa

81.8 ± 4.3

45.7 ± 3.1

26.5 ± 8.9

18.1 ± 0.4

5.0 ± 0.4

3.9 ± 0.6

[225Ac(phospa)]3− (n = 3)

0

0

NDa

NDa

NDa

NDa

NDa

[225Ac(DOTA)] (n = 2)

95.2 ± 3.3

94.5 ± 3.5

94.9 ± 2.9

86.2 ± 3.1

NDa

NDa

77.1 ± 3.6

[225Ac(macropa)]+ (Thiele et al. 2017)

95

NDa

93

92

91

93

91b

[225Ac(bispa2)]+ (Comba et al. 2017)

NDa

95.5 ± 0.2

91.5 ± 0.7

88.8 ± 2.5

85.2 ± 1.7

74.4 ± 1.4

71.1 ± 2.7

  1. aND not determined. b8 d time point