Indimitecan

Indimitecan (LMP776) is a topoisomerase I (Top1) inhibitor with anticancer activities[1].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

Top1

Indimitecan (LMP776) (0-100 μM) shows antiproliferative potencies against various human cancer cell lines, with mean-graph midpoint (MGM) of 0.079 ± 0.023 μM[1]. Indimitecan shows potent DNA cleavage due to Top1 inhibition[1]. Indimitecan can be substrates for metabolic ketone reductases[1]. Cell Proliferation Assay[1] Cell Line: HOP-62, HCT-116, SF-539, UACC-62, OVCAR-3, SN12C, DU-145, MCF-7 Concentration: 0-100 μM Incubation Time: Result: Showed growth inhibition with GI50s of <0.01, <0.01, 0.04, <0.01, 0.08, <0.01, <0.01 and 0.01 μM against HOP-62, HCT-116, SF-539, UACC-62, OVCAR-3, SN12C, DU-145 and MCF-7 cells, respectively. And the mean-graph midpoint (MGM) for growth inhibition of all human cancer cell lines successfully tested (the National Cancer Institute’s developmental therapeutics assay (the “NCI60”)) was 0.079 ± 0.023 μM.

[1]. Cinelli MA, et al. Identification, synthesis, and biological evaluation of metabolites of the experimental cancer treatment drugs indotecan (LMP400) and indimitecan (LMP776) and investigation of isomerically hydroxylated indenoisoquinoline analogues as topoisomerase I poisons. J Med Chem. 2012 Dec 27;55(24):10844-62.