Azide-PEG4-Val-Cit-PAB-SN-38 serves as a cleavable ADC linker conjugated to SN-38, an anti-tumor drug and active metabolite of irinotecan. SN-38 inhibits DNA topoisomerase I, halting DNA synthesis and causing single-strand breaks. The Val-Cit linker is cleaved by lysosomal Cathepsin B, ensuring targeted intracellular release. The azide group participates in copper-catalyzed click chemistry with alkyne, DBCO, and BCN. The PEG spacer imparts water solubility to the molecule and helps optimize DMPK properties.
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