A DNA topoisomerase I inhibitor; exhibits selective cytotoxicity across a panel of 46 NSCLC lines (IC50s = ~2 μM for HCC4017

SW044248 – 5 mg

Brand:
Cayman
CAS:
522650-83-5
Storage:
-20
UN-No:
Non-Hazardous - /

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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SKU: 23459 - 5 mg Category:

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

Formal name: 2-[(5-ethyl-5H-1,2,4-triazino[5,6-b]indol-3-yl)thio]-N-(2-methoxyphenyl)-butanamide

Synonyms: 

Molecular weight: 421.5

CAS: 522650-83-5

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Topoisomerases||Research Area|Cancer|Cell Death||Research Area|Cancer|DNA Damage and Repair

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