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Amrubicin

CAS No. : 110267-81-7

MCE 站：Amrubicin

产品活性：Amrubicin (SM-5887) 是一种 DNA 拓扑异构酶 II (topoisomerase II) 抑制剂，可用于癌症研究。

研究领域：Cell Cycle/DNA Damage

作用靶点：Topoisomerase

In Vitro: Amrubicin (SM-5887) is a DNA topoisomerase II inhibitor. Amrubicin (SM-5887) (2.5 μg/mL) shows radio-enhancement effects on human lung adenocarcinoma A549 cells. Amrubicin supresses the LX-1, A549, A431, and BT-474 cell lines, with IC₅₀s of 1.1 ± 0.2, 2.4 ± 0.8, 0.61 ± 0.10 and 3.0 ± 0.3 ?g/mL, respectively. Amrubicin inhibits the cell cycle profile of U937 cells with an IC₅₀ of 5.6 ?M. Amrubicin (SM-5887) (20 ?M) also induces apoptosis in U937 cells, activates caspase-3/7 and reduces the mitochondrial membrane potential (Δψm).

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.

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