Tumor0.52 ± 0.050.79 ± 0.210.41 ± 0.112.68 ± 0.720.39 ± 0.110.56 ± 0.170.36 ± 0.122.65 ± 0.50
a%ID/g ± SD.Full-size table
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FIG. 5.
Comparison of tumor and muscle uptake at 2 h of 201Tl, 99mTc-MIBI, 99mTc-EIBI, and 99mTc-MMBI in A-549, BT-20, and CX-1 subcutaneous, CX-1 subrenal capsule, and CX-1 hepatic tumor xenograft models.
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Discussion
In AZD 7762 present study we evaluated lipophilicity, in vitro cell accumulation, and in vivo biodistribution of a series of 99mTc-ether isonitrile complexes, the goal being to determine whether increased lipophilicity enhances extraction efficiency by tumor and/or background clearance.
Lipophilicity constants were determined by HPLC for each 99mTc-isonitrile compound by linear extrapolation to 0% methanol (Table 2). This extrapolation method was necessary because there was no one particular methanol–buffer concentration where the retention times of all ten 99mTc-isonitriles were measurable with reverse-phase HPLC.