ADC | Time | Free PBD-dimer 3 | Cyclopropyl thiol 4 | ||||||
---|---|---|---|---|---|---|---|---|---|
Tumor | Liver | Kidney | Lung | Tumor | Liver | Kidney | Lung | ||
hours | pmol/g | pmol/g | |||||||
Cyclobutyl-containing ADC 1 | 24 | 1.03 | 0.26 | 0.30 | 0.96 | ND | ND | ND | ND |
2.10 | 0.55 | 0.30 | 0.76 | ND | ND | ND | ND | ||
96 | 1.94 | <LLOQ | <LLOQ | 0.38 | ND | ND | ND | ND | |
2.06 | <LLOQ | <LLOQ | 0.32 | ND | ND | ND | ND | ||
Cyclopropyl-containing ADC 2 | 24 | ND | ND | ND | ND | 7.58 | 1.42 | 1.47 | 1.78 |
ND | ND | ND | ND | 6.77 | 0.63 | 1.03 | 1.72 | ||
96 | <LLOQ | ND | ND | ND | 4.34 | <LLOQ | 0.33 | 0.67 | |
ND | <LLOQ | <LLOQ | ND | 4.69 | 0.33 | 0.37 | 1.06 |
The free payload concentration results in tumor and liver were published previously (Zhang et al., 2016a) and were included here for comparison only. LLOQ, 0.244 nM for PBD-dimer 3 and cyclopropyl thiol 4 in tissue homogenates; ND, not detected.