Abstract
[18/19F]-4, an anionic GCPII/PSMA inhibitor for image-guided intervention in prostate cancer, is described. [19F]-4 is radiolabeled with a radiochemical yield that is ≥27% and a molar activity of 190 ± 50 mCi/μmol in a <1 h, one-step, aqueous isotopic exchange reaction. [19F]-4 allows PSMA expression to be imaged by fluorescence (FL) and [18F]-PET. PC3-PIP (PSMA-positive, EC50 = 6.74 ± 1.33 nM) cancers are specifically delineated in mice that bear 3 million (18 mg) PC3-PIP and PC3 (control, PSMA-negative) cells. Colocalization of [18/19F]-4 PET, fluorescence, scintillated biodistribution, and PSMA expression are observed.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 4256-4262 |
| Number of pages | 7 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 61 |
| Issue number | 9 |
| DOIs | |
| State | Published - May 10 2018 |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery
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