Article Figures & Data
Figures
- FIGURE 1.
Structure of bombesin and 64Cu-labeled bombesin analogs.
- FIGURE 2.
Competitive binding assay of Cu-DOTA-8-AOC-BBN(7–14)NH2 and Cu-CB-TE2A-8-AOC-BBN(7–14)NH2 analogs vs. [125I-Tyr4]BBN using PC-3 cells (n = 3).
- FIGURE 3.
Internalization of 64Cu-CB-TE2A-8-AOC-BBN(7–14)NH2 using PC-3 cells (n = 6).
- FIGURE 4.
Internalization of 64Cu-DOTA-8-AOC-BBN(7–14)NH2 using PC-3 cells (n = 2).
- FIGURE 5.
Comparison of 64Cu-CB-TE2A-8-AOC-BBN(7–14)NH2 (red) and 64Cu-DOTA-8-AOC-BBN(7–14)NH2 (yellow) using a radiolocalization index ([RI] %ID/g of tumor/%ID/g of nontarget tissue).
- FIGURE 6.
mircoPET, fused microPET/CT, and axial images of 64Cu-DOTA-8-AOC-BBN(7–14)NH2 (A) and 64Cu-CB-TE2A-8-AOC-BBN(7–14)NH2 (B) in PC-3 tumor-bearing SCID mice at 20 h after administration. Lateral and axial projection images have been normalized to the highest pixel intensity for each respective image.
Tables
Analog Molecular formula MS calculated MS observed RP-HPLC tr (min)* IC50 (nM)† DOTA-8-AOC-BBN(7–14)NH2 C67H106N18O17S 1,467.8 1,468.0 13.8 Cu-DOTA-8-AOC-BBN(7–14)NH2 C67H104N18O17SCu 1,528.7 1,528.5 15.0 1.44 ± 0.08 CB-TE2A-8-AOC-BBN(7–14)NH2 C67H108N18O13S 1,405.8 1,405.8 15.8 0.67 ± 0.07 Cu-CB-TE2A-8-AOC-BBN(7–14)NH2 C67H106N18O13SCu 1,465.7 1,465.7 17.2 0.48 ± 0.01 - TABLE 2
In Vivo Pharmacokinetic Studies of 64Cu-DOTA-8-AOC-BBN(7–14)NH2 Using SCID Mice Bearing PC-3 Xenografts
Tissue/organ 15 min 1 h 4 h 24 h Blood 3.18 ± 0.91 1.22 ± 0.62 0.76 ± 0.46 0.90 ± 0.48 Heart 3.36 ± 1.06 2.05 ± 1.45 1.63 ± 0.73 2.69 ± 1.09 Lung 5.19 ± 1.76 2.96 ± 1.84 3.27 ± 1.31 3.55 ± 1.17 Liver 14.97 ± 3.37 9.56 ± 5.20 8.98 ± 2.74 7.80 ± 1.51 Stomach 3.94 ± 0.70 2.30 ± 0.96 2.46 ± 0.95 1.68 ± 0.59 Small intestines 8.26 ± 3.55 13.45 ± 2.08 5.04 ± 1.07 2.84 ± 0.48 Large intestines 5.13 ± 3.25 5.58 ± 2.84 16.29 ± 3.81 3.78 ± 0.85 Kidneys 15.16 ± 2.99 8.46 ± 2.79 5.43 ± 0.90 4.58 ± 0.95 Spleen 2.68 ± 1.60 2.52 ± 1.59 3.57 ± 2.23 3.59 ± 2.48 Pancreas 23.30 ± 4.43 13.81 ± 2.69 12.16 ± 1.34 3.65 ± 0.44 Muscle 1.23 ± 0.14 0.65 ± 0.37 0.26 ± 0.14 0.46 ± 0.21 Bone 1.98 ± 0.51 1.12 ± 0.66 0.79 ± 0.35 1.15 ± 0.59 Tumors 4.95 ± 0.91 3.48 ± 0.90 3.00 ± 1.10 3.88 ± 1.40 Excretion (%ID) 19.13 ± 6.94 44.63 ± 9.15 49.77 ± 8.19 67.84 ± 5.43 All data, except excretion, are presented as %ID/g ± SD. Excretion data are presented as %ID ± SD (n = 5).
- TABLE 3
In Vivo Pharmacokinetic Studies of 64Cu-CB-TE2A-8-AOC-BBN(7–14)NH2 Using SCID Mice Bearing PC-3 Xenografts
Tissue/organ 15 min 1 h 4 h 24 h Blood 2.37 ± 1.47 0.51 ± 0.14 0.06 ± 0.05 0.05 ± 0.03 Heart 1.45 ± 0.67 0.09 ± 0.08 0.08 ± 0.08 0.10 ± 0.09 Lung 2.86 ± 1.12 0.60 ± 0.19 0.22 ± 0.15 0.15 ± 0.08 Liver 5.52 ± 1.32 2.15 ± 0.26 0.64 ± 0.08 0.21 ± 0.06 Stomach 2.56 ± 0.62 0.94 ± 0.27 1.65 ± 2.63 0.05 ± 0.04 Small intestines 12.88 ± 2.06 13.17 ± 1.21 1.78 ± 0.57 0.11 ± 0.04 Large intestines 4.27 ± 0.97 3.52 ± 1.12 17.70 ± 7.06 0.20 ± 0.08 Kidneys 21.66 ± 8.58 5.26 ± 0.58 1.88 ± 0.53 0.28 ± 0.22 Spleen 2.96 ± 2.84 0.68 ± 0.53 0.16 ± 0.16 0.56 ± 0.30 Pancreas 31.28 ± 3.24 17.66 ± 2.00 2.18 ± 0.71 0.18 ± 0.14 Muscle 0.88 ± 0.38 0.26 ± 0.15 0.10 ± 0.07 0.22 ± 0.17 Bone 2.15 ± 2.01 0.58 ± 0.41 0.39 ± 0.25 0.29 ± 0.10 Tumors 6.95 ± 2.27 2.65 ± 1.05 1.32 ± 0.49 0.28 ± 0.21 Excretion (%ID) 26.48 ± 10.18 60.38 ± 2.16 77.88 ± 6.58 98.60 ± 0.28 All data, except excretion, are presented as %ID/g ± SD. Excretion data are presented as %ID ± SD (n = 5).
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