SN-38

拓扑异构酶I的抑制剂和伊立替康的活性代谢物；在无细胞测定中，浓度为0.1、1和10µM时诱导拓扑异构酶I依赖性DNA裂解；在200nM时诱导HT-29细胞中的DNA单链断裂；在HT-29细胞中诱导细胞毒性（IC50=8.8nM）；在MX-1乳腺癌小鼠异种移植模型中，每天100mg/kg时可减小肿瘤体积而不影响体重。An inhibitor of topoisomerase I and an active metabolite of irinotecan; induces topoisomerase I-dependent DNA cleavage in a cell-free assay at 0.1, 1, and 10 µM; induces DNA single-strand breaks in HT-29 cells at 200 nM; induces cytotoxicity in HT-29 cells (IC50 = 8.8 nM); reduces tumor volume without affecting body weight in an MX-1 breast cancer mouse xenograft model at 100 mg/kg per day.