Description
A DNA topoisomerase I inhibitor; exhibits selective cytotoxicity across a panel of 46 NSCLC lines (IC50s = ~2 µM for HCC4017, H292, and H1819 cells versus >20 µM for the remaining cell lines); induces cleavage of PARP and caspase-3 and blocks DNA replication, RNA transcription, and protein translation in susceptible-, but not resistant-, cells in a dose-dependent manner; inhibits the ability of recombinant topoisomerase 1 to relax supercoiled DNA; topoisomerase 1 knockdown rescues HCC4017 cells from SW04428 cytotoxicity; expression of CDKN1A reduces SW044248 cytotoxicity