MC-SN38 是一种由有效的微管破坏剂 SN38 和不可切割的 MC linker 组成的药物偶联物，用于合成抗体药物偶联物 (ADC)。SN-38 是拓扑异构酶 I 抑制剂伊立替康的活性代谢物，抑制 DNA 合成，导致 DNA 单链断裂。
MC-SN38 is a drug-linker conjugate composed of a potent microtubule-disrupting agent SN38 and a non-cleavable MC linker to make antibody drug conjugate (ADC). SN-38, an active metabolite of the Topoisomerase I inhibitor Irinotecan, inhibits DNA synthesis and causes frequent DNA single-strand breaks[1][2].
[1]. Jensen NF, et al. Characterization of DNA topoisomerase I in three SN-38 resistant human colon cancer cell lines reveals a newpair of resistance-associated mutations. J Exp Clin Cancer Res. 2016 Mar 31;35:56.
[2]. Kawato Y, et al. Intracellular roles of SN-38, a metabolite of the camptothecin derivative CPT-11, in the antitumor effect of CPT-11. Cancer Res. 1991;51(16):4187-4191.
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