Table 2.
The average of tumour-to-kidneys absorbed dose ratios considering different combinations kon and koff, ligand amounts and λint.
| KDa [nM] | koffb[1/ min] | konc[L/ nmol/min] | Ligand amount [nmol] | Tumour-to-kidneys absorbed dose ratio of… | |||||
|---|---|---|---|---|---|---|---|---|---|
| Tumour 1 and 2 for λintd of… | Tumour REST for λintd of… | ||||||||
| 0.01 [min−1] | 0.001 [min−1] | 0.0001 [min−1] | 0.01 [min−1] | 0.001 [min−1] | 0.0001 [min−1] | ||||
| 0.01 | 0.0001 | 0.01 | 32 | 1.8 ± 1.3 | 2.3 ± 1.7 | 2.4 ± 1.7 | 1.3 ± 1.0 | 1.8 ± 1.4 | 2.2 ± 1.6 |
| 100 | 2.2 ± 1.6 | 3.1 ± 2.3 | 3.1 ± 2.2 | 1.7 ± 1.4 | 3.1 ± 2.2 | 3.7 ± 2.6 | |||
| 316 | 2.9 ± 2.1 | 3.5 ± 2.4 | 3.2 ± 2.1 | 2.7 ± 2.0 | 4.2 ± 2.8 | 4.2 ± 2.6 | |||
| 0.01 | 0.001 | 0.1 | 32 | 1.2 ± 0.9 | 2.2 ± 1.7 | 3.0 ± 2.3 | 0.8 ± 0.6 | 1.6 ± 1.4 | 2.7 ± 2.1 |
| 100 | 1.8 ± 1.4 | 3.1 ± 2.3 | 3.4 ± 2.4 | 1.3 ± 1.1 | 3.1 ± 2.2 | 4.2 ± 3.0 | |||
| 316 | 2.6 ± 1.9 | 3.4 ± 2.4 | 3.4 ± 2.3 | 2.3 ± 1.7 | 4.1 ± 2.8 | 4.6 ± 2.9 | |||
| 0.1 | 0.001 | 0.01 | 32 | 1.8 ± 1.3 | 2.6 ± 1.9 | 3.2 ± 2.3 | 1.4 ± 1.1 | 2.3 ± 1.7 | 3.6 ± 2.4 |
| 100 | 2.2 ± 1.7 | 3.4 ± 2.5 | 3.5 ± 2.4 | 1.8 ± 1.4 | 3.5 ± 2.5 | 4.7 ± 3.1 | |||
| 316 | 2.9 ± 2.1 | 3.6 ± 2.5 | 3.4 ± 2.3 | 2.7 ± 2.0 | 4.5 ± 3.0 | 4.8 ± 3.0 | |||
| 0.1 | 0.01 | 0.1 | 32 | 1.3 ± 1.0 | 2.8 ± 2.1 | 3.7 ± 2.6 | 0.9 ± 0.7 | 2.3 ± 1.8 | 4.2 ± 2.9 |
| 100 | 1.9 ± 1.4 | 3.5 ± 2.6 | 3.8 ± 2.6 | 1.4 ± 1.2 | 3.7 ± 2.7 | 5.1 ± 3.3 | |||
| 316 | 2.7 ± 1.9 | 3.7 ± 2.6 | 3.5 ± 2.4 | 2.4 ± 1.8 | 4.6 ± 3.1 | 5.0 ± 3.1 | |||
| 1 | 0.01 | 0.01 | 32 | 2.1 ± 1.6 | 3.4 ± 2.4 | 3.3 ± 2.2 | 1.7 ± 1.3 | 3.7 ± 2.5 | 4.3 ± 2.7 |
| 100 | 2.5 ± 1.9 | 3.7 ± 2.6 | 3.3 ± 2.2 | 2.1 ± 1.6 | 4.4 ± 3.0 | 4.6 ± 2.9 | |||
| 316 | 3.0 ± 2.2 | 3.7 ± 2.6 | 3.1 ± 2.0 | 3.0 ± 2.1 | 4.9 ± 3.2 | 4.4 ± 2.7 | |||
| 1 | 0.1 | 0.1 | 32 | 1.8 ± 1.4 | 3.5 ± 2.5 | 3.4 ± 2.3 | 1.4 ± 1.1 | 3.7 ± 2.6 | 4.4 ± 2.8 |
| 100 | 2.3 ± 1.7 | 3.8 ± 2.7 | 3.3 ± 2.3 | 1.9 ± 1.5 | 4.5 ± 3.1 | 4.7 ± 2.9 | |||
| 316 | 2.9 ± 2.1 | 3.8 ± 2.6 | 3.1 ± 2.0 | 2.8 ± 2.0 | 4.9 ± 3.2 | 4.4 ± 2.7 | |||
aKD = Dissociation constant (KD = koff/kon); bkoff = Dissociation rate; ckon = Association rate; dλint = Internalization rate. The values in bold are the maximum tumour-to-kidneys absorbed dose ratio.