A DNA topoisomerase I inhibitor
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SW044248

Item No. 23459

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(5-ethyl-5H-1,2,4-triazino[5,6-b]indol-3-yl)thio]-N-(2-methoxyphenyl)-butanamide
CAS Number
522650-83-5
Molecular Formula
C22H23N5O2S
Formula Weight
421.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 5 mg/mlEthanol: 1 mg/ ml
λmax
202, 267, 344 nm
SMILES
CCN1C2=NC(SC(CC)C(NC3=C(OC)C=CC=C3)=O)=NN=C2C4=CC=CC=C14
InChi Code
InChI=1S/C22H23N5O2S/c1-4-18(21(28)23-15-11-7-9-13-17(15)29-3)30-22-24-20-19(25-26-22)14-10-6-8-12-16(14)27(20)5-2/h6-13,18H,4-5H2,1-3H3,(H,23,28)
InChi Key
PEVRGVRHMMZNGI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $70

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    10 mg

    $125

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    25 mg

    $241

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    50 mg

    $412

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    Cayman Chemical
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    Product Description

    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).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Zubovych, I.O., Sethi, A., Kulkarni, A., et al. A novel inhibitor of topoisomerase I is selectively toxic for a subset of non-small cell lung cancer cell lines. Mol. Cancer Ther. 15(1), 23-36 (2016).