Table 1 IC50 values of different metal-chelate conjugates consisting of cyclo(-d-Tyr-N-Me-d-Orn(spacer-[M 3+ ]chelator)-l-Arg-l-2-Nal-Gly-), expressed as mean ± SD (n = 3)
From: The influence of different metal-chelate conjugates of pentixafor on the CXCR4 affinity
Compound | IC50/nM | Compound | IC50/nM |
|---|---|---|---|
1 (DOTA) | 102 ± 17 | 2 (DOTAGA) | 654 ± 263 |
[natGa3+]1 | 24.8 ± 2.5 | [natGa3+]2 | 380 ± 102 |
[natBi3+]1 | 22.1 ± 7.0 | [natBi3+]2 | 29.4 ± 7.6 |
[natCu2+]1 | 131 ± 11 | [natCu2+]2 | 1165 ± 220 |
[natLu3+]1 | 40.9 ± 12 | [natLu3+]2 | 188 ± 2.8 |
[natY3+]1 | 40.8 ± 27 | [natY3+]2 | 126 ± 89 |
3 (NOTA) | 253 ± 49 | 4 (NODAGA) | 275 ± 106 |
[natGa3+]3 | 17.8 ± 7.7 | [natGa3+]4 | 342 ± 72 |
[natCu2+]3 | 46.1 ± 26 | [natCu2+]4 | 343 ± 10 |
[natF]AlF-3 | 220 ± 57 | ||
5 (SCN-Bn-NODA) | 115 ± 24 | 6 (DTPA) | 53 ± 7.9 |
[natF]AlF-5 | 329 ± 49 | [natY3+]6 | 156 ± 6.7 |
7 (SCN-Bn-DTPA) | 200 ± 73 | [natLu3+]6 | 111 ± 77 |
[natIn3+]7 | 74.1 ± 2.4 | [natIn3+]6 | 90 ± 42 |
8 (SCN-Bn-DFO) | 105 ± 35 | [natCu2+]6 | 175 ± 66 |
[natZr4+]8 | 148 ± 27 |