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Lapcin

Chemical Structure : Lapcin

CAS No.:

Lapcin

Catalog No.: PC-38245Not For Human Use, Lab Use Only.

Lapcin is a potent dual topoisomerase I/II inhibitor with nM to pM IC50s against diverse cancer cell lines (Colon cancer HT29 cell IC50=0.516 nM).

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    Biological Activity

    Lapcin is a potent dual topoisomerase I/II inhibitor with nM to pM IC50s against diverse cancer cell lines (Colon cancer HT29 cell IC50=0.516 nM).
    Lapcin showed weak activity against DNA gyrase (IC50>20.5 uM).
    While only weakly active against DNA gyrase, lapcin was a potent of inhibitor of both DNA relaxation by topoisomerase I (IC50=2.17 uM) and DNA decatenation by topoisomerase II (IC50=7.53uM), 14 times more potent than the alkaloid camptothecin.
    Lapcin was more potent than the topoisomerase II inhibitor etoposide against all of the cell lines we tested, with the exception of the lung cancer cell NCI-H226, against which it was essentially equipotent.
    Cell lines expressing wild-type p53 (HCT116, H226, MCF7) tended to show higher IC50s than p53 reduced cell lines (NCI-H1299, HT29, Colo205, Hela).

    Physicochemical Properties

    M.Wt 1304.502
    Formula C64H77N11O15S2
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    4-(4-(4-((2S)-4-amino-2-(2'-(4-((2S)-2-((2S)-3-hydroxy-2-((2S)-2-(3-hydroxytetradecanamido)propanamido)propanamido)propanamido)phenyl)-[2,4'-bithiazole]-4-carboxamido)-4-oxobutanamido)benzamido)-2-hydroxy-3-isopropoxybenzamido)benzoic acid

    References

    1. Wang Z, et al. Nat Commun. 2022 Feb 11;13(1):842. 

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