Indimitecan (LMP776) 是一种具有抗癌活性的拓扑异构酶 I（Top1）抑制剂。

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

Indimitecan (LMP776) (0-100 μM) demonstrates 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 GI 50 s 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.

915360-05-3

C25H21N3O6

459.45

LMP776

DMSO:7.7mg/mL (16.7mM),ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years