Table 1.
Analytical data for NOTA-BBN(6-14) monomer and dimmers
| Peptide | [M]+ | Yield | Purityb | Kic | Labeling | |
|---|---|---|---|---|---|---|
| Calcd | Founda | (%) | (%) | (nM) | yieldd (%) | |
| Bombesin | 0.59 ± 0.32 | |||||
| NOTA-monomer | 1,570 | 1,571 | 38 | 99 | 2.51 ± 1.54e | > 95 |
| South BBN peptide segment | 1,879 | 1,880 | 84f | |||
| NOTA-dimer 1 | 2,976 | 2,976 | 28 | 99 | 2.00 ± 1.59 | > 95 |
| NOTA-dimer 2 | 3,122 | 3,122 | 31 | 99 | 1.76 ± 1.30 | > 95 |
aMass values were obtained by MALDI TOF mass spectroscopy or LC/MS/MS. bPurity was determined by HPLC analysis. cAffinities for GRPR were determined with [125I-Tyr4]bombesin in PC3 human prostate cancer cell line. dLabeling yield (not decay-corrected) was determined by radio-HPLC analysis based on 64Cu starting activity. eSimilar Ki values were obtained for the free chelate (1.30 ± 0.74) and the 'cold' Cu/NOTA-monomer (1.60 ± 0.59) when tested in triplicate in human breast cancer T47D cells. fHPLC yield of the crude peptide. NOTA, 1,4,7-triazacyclononane-1,4,7-triacetic acid; Ki, inhibition constant.