Lapcin

Chemical Structure : Lapcin

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货号: 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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生物&药学活性

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).

物理化学性质&存储条件

分子量	1304.502
分子式	C64H77N11O15S2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

Lapcin

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物理化学性质&存储条件

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Lapcin

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