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Lapcin

  Cat. No.:  DC70557  
Chemical Structure
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More than 5000 active chemicals with high quality for research!
Field of application
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).
Cas No.:
Chemical Name: Lapcin
Formula: C64H77N11O15S2
M.Wt: 1304.502
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC7131 GENZ-644282 Genz-644282 is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity(IC50=1.2 nM).
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DC76266 β-Glu-PAB(CH2NH2)-Exatecan β-Glu-PAB(CH2NH2)-Exatecan (Compound 9a) is a topoisomerase I inhibitor. β-Glu-PAB(CH2NH2)-Exatecan binds to the topoisomerase I-DNA complex to prevent DNA strand reconnection, thereby inducing DNA breakage and cell apoptosis. β-Glu-PAB(CH2NH2)-Exatecan can be specifically cleaved by β-glucuronidase highly expressed in the tumor microenvironment to release Exatecan for cytotoxic effect. β-Glu-PAB(CH2NH2)-Exatecan is also an intermediate of Mal((3S,3aR,6S,6aR) -hexahydrofuro [3, 2-B]furan-3,6-diamine-PEG12)-β -Glu-Pab-Exatecan. β-Glu-PAB(CH2NH2)-Exatecan is promising for research of cancers.
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DC76263 Mal-Exatecan Mal-Exatecan is a Mal (Maleimide) modified Exatecan. Rilpivirine is an effective and selective diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). It exhibits potent antiviral activity against both wild-type HIV (EC50 = 0.4 nM) and mutant strains (EC50 = 0.1-2.0 nM).
DC76262 GGFG-PAB-Exatecan TFA GGFG-PAB-Exatecan TFA consists of an ADC toxin Exatecan-induced allodynia and in PGE2-induced mechanical hyperalgesia. AD353 exhibits a favorable pharmacokinetic profile.
DC76261 Fostriecin Fostriecin is a triene antibiotic. Fostriecin is a topoisomerase II and protein phosphatase PP2A inhibitor.
DC76260 AuL1 AuL1 is an inhibitor of topoisomerase IIα (Top II) with DNA-intercalating properties. AuL1 is cytotoxic to tumor cells and can be used in the research of anticancer agents.
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