Table 1.
Physiochemical properties of radiolabeled SAHA-based HDAC ligands.
| Compound | MW | Log D | RCY | Target | IC50 for HDACs | In Vivo Properties in Rodents | Reference |
|---|---|---|---|---|---|---|---|
| [18F]1 | 265.32 | 1.39 | 11–15% | Class IIa | – | Brain uptake: 0.44 and 0.40% ID/g at 5 and 60 min, respectively (rat) |
[26,43,44,46] |
| [18F]2 | 283.31 | – | 25% | Class IIa | – | Brain uptake: SUVs were around 1 in various brain regions during the 60-min scan (rat) |
[57] |
| [18F]3 | 301.30 | – | 22% | Class IIa | – | Brain uptake: SUVs were around 1 in various brain regions during the 60-min scan (rat) |
[57] |
| [18F]4 | 309.37 | 1.01 | 19% | Non-selective | HDAC1: 56 nM HDAC5: 67 nM HDAC6: 3 nM HDAC7: 85 nM |
Brain uptake: 1.0, 0.7, and 0.4% ID/g at 30, 60, and 120 min, respectively Defluorination: 9.6, 11.1, and 13.4% ID/g bone uptake at 30, 60, and 120 min, respectively (tumor-bearing mouse) |
[58] |
| [18F]5 | 281.32 | – | 40% | HDAC1–3/6 | HDAC1: 9.0 nM HDAC2: 13 nM HDAC3: 24 nM HDAC6: 50 nM |
Brain uptake: Very limited in biodistribution study (mouse/tumor-bearing mouse) |
[59] |
| [11C]6 | 278.34 | 0.5 | 23% | – | – | – | [60] |
| [11C]7 | 247.33 | 1.7 1 | 48% | – | – | – | [60] |
1 Clog P. MW: molecular weight; RCY: radiochemical yield (decay corrected); SUV: standardized uptake value; ID: injected dose.