Table 1. Biodistribution and Tumor-to-Normal Tissue Ratios of 68Ga-Labeled CCZ01099 in Male C57BL/6J Mice Bearing B16–F10 Melanoma at 1 and 2 h p.i. Blocking was Performed by Co-Injection of 0.5 mg of MC1R-Specific Inhibitor BMS 470539 (Two-Way ANOVA Analysis was Performed Comparing 1 h p.i. vs 1 h p.i. Blocked, Multiple Comparisons Were Corrected Using the Holm–Sidak Method, *p < 0.05, ***p < 0.001)a.
tissue | 1 h p.i. unblocked (n = 5) | 2 h p.i. unblocked (n = 4) | 1 h p.i. blocked (n = 5) |
---|---|---|---|
B16F10 tumor | 6.33 ± 1.48 | 5.22 ± 1.30 | 0.60 ± 0.15*** |
blood | 0.65 ± 0.12 | 0.19 ± 0.01 | 0.27 ± 0.04 |
fat | 0.09 ± 0.04 | 0.02 ± 0.01 | 0.04 ± 0.02 |
seminal glands | 0.11 ± 0.06 | 0.04 ± 0.01 | 0.07 ± 0.03 |
testes | 0.20 ± 0.06 | 0.07 ± 0.01 | 0.10 ± 0.02 |
intestine | 0.34 ± 0.07 | 0.53 ± 0.38 | 0.17 ± 0.05 |
spleen | 0.35 ± 0.08 | 0.19 ± 0.03 | 0.52 ± 0.28 |
pancreas | 0.17 ± 0.04 | 0.07 ± 0.01 | 0.08 ± 0.01 |
stomach | 0.22 ± 0.11 | 0.20 ± 0.16 | 0.19 ± 0.12 |
liver | 0.53 ± 0.07 | 0.44 ± 0.08 | 0.38 ± 0.11 |
adrenal glands | 0.79 ± 0.72 | 0.33 ± 0.19 | 0.45 ± 0.29 |
kidneys | 5.59 ± 0.88 | 4.42 ± 0.55 | 2.62 ± 0.91*** |
heart | 0.24 ± 0.06 | 0.08 ± 0.01 | 0.13 ± 0.02 |
lungs | 0.69 ± 0.11 | 0.31 ± 0.05 | 0.34 ± 0.13 |
thyroid | 0.30 ± 0.08 | 0.16 ± 0.03 | 0.13 ± 0.05 |
bone | 0.33 ± 0.18 | 0.10 ± 0.03 | 0.17 ± 0.10 |
muscle | 0.16 ± 0.05 | 0.04 ± 0.00 | 0.08 ± 0.03 |
brain | 0.05 ± 0.04 | 0.01 ± 0.00 | 0.03 ± 0.02 |
tumor to normal tissue ratios | |||
tumor/muscle | 40.6 ± 11.9 | 125 ± 29.6 | 7.98 ± 1.35*** |
tumor/blood | 9.94 ± 2.93 | 27.7 ± 5.34 | 2.24 ± 0.40 |
tumor/bone | 23.3 ± 12.1 | 52.7 ± 13.4 | 4.19 ± 1.80*** |
tumor/liver | 11.9 ± 2.26 | 11.8 ± 2.72 | 1.79 ± 0.88* |
tumor/kidneys | 1.13 ± 0.22 | 1.21 ± 0.44 | 0.26 ± 0.12 |
Values are in percentage of injected dose per gram of tissue (%ID/g, mean ± standard deviation).