Background
Methods
Results
Compound | logP | IC50 (nM) | Total cellular activity 1 h (%) | Internalized activity 1 h (%) |
---|---|---|---|---|
NOTA-pentixafor | – | 253 ± 49 | – | – |
[68Ga]NOTA-pentixafor | −2.36 | 17.8 ± 7.7 | 2.45 ± 0.02 | 0.43 ± 0.07 |
Pentixafor | – | 102 ± 17 | – | – |
[68Ga]pentixafor | −2.90 | 24.8 ± 2.5 | 6.36 ± 0.46 | 3.39 ± 0.16 |
Organ | Tracer | ||
---|---|---|---|
[68Ga]NOTA-pentixafor (n = 5) | [68Ga]NOTA-pentixafor + AMD3100 (n = 3) | [68Ga]pentixafor (n = 6) | |
Blood | 0.65 ± 0.41 | 0.62 ± 0.26 | 0.97 ± 0.34 |
Heart | 0.34 ± 0.19 | 0.36 ± 0.14 | 0.58 ± 0.17 |
Lung | 0.73 ± 0.25 | 0.95 ± 0.38 | 1.32 ± 0.29 |
Liver | 2.30 ± 0.88 | 2.02 ± 0.76 | 2.05 ± 0.27 |
Gallbladder | 3.61 ± 3.00 | 5.14 ± 2.24 | |
Pancreas | 0.12 ± 0.05 | 0.16 ± 0.05 | 1.06 ± 0.22 |
Spleen | 0.44 ± 0.22 | 0.54 ± 0.19 | 0.30 ± 0.10 |
Kidney | 2.71 ± 1.06 | 3.56 ± 1.03 | 1.65 ± 0.91 |
Adrenals | 0.52 ± 0.30 | 0.48 ± 0.15 | 3.68 ± 0.72 |
Stomach | 0.45 ± 0.21 | 0.58 ± 0.24 | 0.48 ± 0.08 |
Intestine | 1.89 ± 0.83 | 3.97 ± 0.92 | 0.67 ± 0.21 |
Muscle | 0.13 ± 0.10 | 0.13 ± 0.05 | 0.19 ± 0.06 |
Bone | 0.25 ± 0.18 | 0.16 ± 0.07 | n/a |
Tumor | 1.71 ± 0.40 | 0.52 ± 0.17 | 16.2 ± 3.82 |
Tumor-to-organ ratio | |||
T/blood | 2.64 ± 1.78 | 16.7 ± 7.05 | |
T/liver | 0.74 ± 0.34 | 7.90 ± 2.13 | |
T/kidney | 0.63 ± 0.29 | 9.81 ± 5.89 | |
T/muscle | 13.0 ± 9.86 | 85.2 ± 33.6 |