Table 1. In Vitro Cytotoxicities of S-Methylated ADC Metabolites and the Oxidation Products of 12a (12a′ and 12a″).
Cell
Line IC50 (M) |
|||
---|---|---|---|
metabolite | H1703 | H1975 | COLO-704 |
12a (n = 5) | 2.3 × 10–12 | 2.5 × 10–12 | 3.0 × 10–12 |
12b (n = 3) | 5.9 × 10–12 | 5.6 × 10–12 | 6.9 × 10–12 |
3b | 3.7 × 10–12 | 4.1 × 10–12 | 5.1 × 10–12 |
12a′ | 3.1 × 10–10 | 8.4 × 10–10 | 8.2 × 10–10 |
12a″ | 6.3 × 10–10 | 2.1 × 10–10 | 3.6 × 10–10 |