Formulation: A crystalline solid
Formal Name: 2-[(5-ethyl-5H-1,2,4-triazino[5,6-b]indol-3-yl)thio]-N-(2-methoxyphenyl)-butanamide
Purity: ≥98%
Formula Markup: C22H23N5O2S
Formula Weight: 421,5
Shelf life (days): 1460
CAS Number: 522650-83-5
Notes: SW044248 is a DNA topoisomerase I inhibitor that exhibits selective cytotoxicity across a panel of 46 non-small cell lung cancer cell (NSCLC) lines (IC50s = ~2 μM for HCC4017, H292, and H1819 cells versus >20 μM for the remaining cell lines).{37220} It induces cleavage of poly(ADP-ribose) polymerase (PARP) and caspase-3 and blocks DNA replication, RNA transcription, and protein translation in HCC4017 susceptible-, but not HBEC30KT resistant-, cells in a dose-dependent manner. SW044248 inhibits the ability of recombinant topoisomerase 1 to relax supercoiled DNA in a dose-dependent manner and topoisomerase 1 knockdown rescues HCC4017 cells from SW044248 cytotoxicity. SW044248 is less cytotoxic against HCC4017 cells transfected with CDKN1, a protein overexpressed in SW044248-resistant NSCLC cells, indicating a role for CDKN1A in SW044248 resistance.
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