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Amrubicin (SM-5887) hydrochloride is a DNA topoisomerase II inhibitor, used for the research of cancer. | [in vivo]
Amrubicin (SM-5887) (25 mg/kg, i.v.) exhibits significant antitumor activities against both SCLC tumors, Lu-24 and Lu-134, with T/C-values (comparing the mean tumor growth rates of the treated group with those of the control group for each day that the tumors are measured) at day 14 of 17% and 9%, respectively. Amrubicin (SM-5887) (25 mg/kg, i.v.) in combination with cisplatin and irinotecan significantly inhibits the growth of tumors compared to amrubicin alone in mice bearing LX-1 tumor cells. Amrubicin (SM-5887) alone or combined with tegafur and uracil also suppresses tumor growth in human cancer xenograft models[2]. | [IC 50]
Topoisomerase II | [References]
[1] Hayashi S, et al. Enhancement of radiosensitivity by topoisomerase II inhibitor, amrubicin and amrubicinol, in human lung adenocarcinoma A549 cells and kinetics of apoptosis and necrosis induction. Int J Mol Med. 2006 Nov;18(5):909-15. PMID:17016621
[2] Hanada M, et al. Amrubicin, a novel 9-aminoanthracycline, enhances the antitumor activity of chemotherapeutic agents against human cancer cells in vitro and in vivo. Cancer Sci. 2007 Mar;98(3):447-54. DOI:10.1111/j.1349-7006.2007.00404.x
[3] Hanada M, et al. Amrubicin induces apoptosis in human tumor cells mediated by the activation of caspase-3/7 preceding a loss of mitochondrial membrane potential. Cancer Sci. 2006 Dec;97(12):1396-403. Epub 2006 Sep 21. DOI:10.1111/j.1349-7006.2006.00318.x |
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