Article Figures & Data
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- FIGURE 1.
Reagents and conditions: 1,5-dibromopentane, NaH, DMF, 50°C, 12 h, 72% (a); silver tosylate, ACN, reflux, 12 h, 96% (b); TBAF, THF, 60°C, 3 h, 84% (c); LiOH/H2O THF/MeOH/H2O (6:3:1), rt, 24 h, 86% (d); and platinum aqua complex, rt, 2 d (e).
- FIGURE 2.
Reagents and conditions: K18F/K222, K2CO3, ACN, 110°C, 10 min (a); 3M NaOH, DCM/MeOH (9:1), 45°C, 30 min (b); 3M HCl (c); and platinum aqua complex, 75°C, 30 min (d).
- FIGURE 3.
HPLC analysis of radiosynthesis steps and purified final product. Sample was run on Waters 4-μm C18 150 × 3.9 mm column (25:75 acetonitrile:0.1% trifluoroacetic acid, at flow rate of 1 mL/min). (A) 18F-FPMA (retention time = 3.38 min). (B) Sample taken from platinum coordination reaction before purification. (C) Sample taken from 18F-FCP product (retention time = 1.43 min).
- FIGURE 4.
Biodistribution of 18F-FCP in KB-3-1 cervical tumor xenograft–bearing adult female nude mice (n = 3/time point) at 5, 30, 60, and 90 min after intravenous injection. Radiotracer uptake in %ID/g was determined by γ-counting.
- FIGURE 5.
HPLC analysis of plasma samples run on Waters 4-μm C18 150 × 3.9 mm column (25:75 acetonitrile:0.1% trifluoroacetic acid, at flow rate of 1 mL/min) at different time points after intravenous injection of 18F-FCP. (A) 5 min. (B) 30 min. (C) 60 min.
- FIGURE 6.
Female nude mouse was injected intravenously with 5.5–6 MBq of 18F-FCP and imaged using Inveon PET/CT scanner (Siemens). (A) Selected slices of dynamic image data that were acquired for up to 90 min. (B) Time–activity curve data generated from dynamic image dataset showing time-dependent kinetics and tissue clearance.
- FIGURE 7.
18F-FCP (5.5–6 MBq) was injected intravenously via tail vein into nude mouse bearing KB-3-1 and COLO-205 xenografts. Imaging was performed 90 min after injection using Inveon PET/CT scanner, and static image was reconstructed and analyzed. Images showed obvious differences in uptake of 18F-FCP between KB-3-1 (2.6 %ID/g) and COLO-205 (0.8 %ID/g) tumors. Furthermore, heterogeneity of uptake was evident in KB-3-1 tumor (inset), showing regions of high (cyan arrow) and low (red arrow) 18F-FCP uptake. This observation is now being further investigated in our laboratory using carboplatin-sensitive (A2780) and carboplatin-resistant (A2780-CP20) tumor models.
Tables
Cisplatin (μM) Carboplatin (μM) 19F-FCP (μM) Cell line 72 h 96 h 72 h 96 h 72 h 96 h COLO-205 25.72 ± 4.32 6.68 ± 7.54 >100 49.37 ± 0.56 69.66 ± 32.33 27.38 ± 5.91 SK-OV-3 12.71 ± 11.84 1.76 ± 0.69 63.92 ± 42.74 17.48 ± 2.06 27.34 ± 9.96 13.21 ± 0.93 FaDu 4.38 ± 2.28 1.22 ± 0.59 45.78 ± 15.65 12.38 ± 1.59 27.53 ± 8.47 8.1 ± 0.64 A549 11.24 ± 0.33 4.95 ± 2.67 59.76 ± 4.53 36.25 ± 6.33 37.74 ± 4.86 26.57 ± 2.51 A498 13.35 5.47 ± 2.90 >100 40.62 ± 1.82 45.73 ± 16.29 21.77 ± 4.62 LNCaP 15.87 ± 4.7 11.34 ± 5.88 >100 74.41 ± 15.57 64.72 ± 21.73 73.83 ± 39.27 KB-3-1 2.98 ± 1.67 3.08 ± 1.48 56.16 ± 5.18 27.28 ± 1.70 19.3 ± 4.89 12.88 ± 0.82 RWPE-1 9.11 ± 4.02 12.83 ± 0.10 88.94 ± 33.59 59.96 ± 1.06 36.23 ± 2.18 39.76 ± 0.40 Data are reported as mean ± SD.
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