Table S1-S7 from Antibody–Exatecan Conjugates with a Novel Self-immolative Moiety Overcome Resistance in Colon and Lung Cancer

Supplementary Table S1 shows cytotoxicity of exatecan compared to DXd. Supplementary Table S2 shows selected hematologic parameters and biochemical parameters from the repeat-dose administration of exatecan mesylate studies in rats. Supplementary Table S3 shows in vitro ADC stability study of total antibody, ADC and free payload. Supplementary Table S4 shows pharmacokinetic parameters of total antibody, ADC and free payload. Supplementary Table S5 shows ADC (T: T-1000-e; D: DS-8201a) internalization rate on cell lines with different HER2 expression level. Supplementary Table S6 shows correlation of exatecan release and target expression. Supplementary Table S7 shows In vitro cytotoxicicity of HER-targeting MTX-1000, TROP2 targeting MTX-132 and HER3-targeting Patritumab-T1000-exatecan and their counterpart DXd-ADC.

补充表S1展示了依喜替康（exatecan）与DXd的细胞毒性；补充表S2展示了大鼠甲磺酸依喜替康重复给药研究中筛选得到的血液学参数与生化参数；补充表S3展示了总抗体、抗体偶联药物（Antibody-Drug Conjugate，ADC）及游离载荷（payload）的体外ADC稳定性研究结果；补充表S4展示了总抗体、ADC与游离载荷的药代动力学参数；补充表S5展示了ADC（T：T-1000-e；D：DS-8201a）在不同人表皮生长因子受体2（Human Epidermal Growth Factor Receptor 2，HER2）表达水平的细胞系上的内化速率；补充表S6展示了依喜替康释放量与靶标表达水平的相关性；补充表S7展示了靶向HER的MTX-1000、靶向滋养层细胞表面抗原2（Trophoblast Cell Surface Antigen 2，TROP2）的MTX-132以及靶向人表皮生长因子受体3（Human Epidermal Growth Factor Receptor 3，HER3）的Patritumab-T1000-依喜替康与其对应的DXd-ADC的体外细胞毒性。