SW044248, CAS 522650-83-5

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.

• Artikelnummer: CAY23459-25
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 23459-25
• Green Labware: Nein
• Verpackungseinheit: 25 mg
• Mengeneinheit: STK
• Methode: Reinstoffe