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. 2019 Sep 27;10(10):1393–1399. doi: 10.1021/acsmedchemlett.9b00310

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