tcsc2837 Amrubicin (hydrochloride)

Amrubicin hydrochloride is a DNA topoisomerase II inhibitor, used for the research of cancer.

IC50 & Target: Topoisomerase II^[1]

In Vitro: Amrubicin hydrochloride is a DNA topoisomerase II inhibitor. Amrubicin (2.5 μg/mL) shows radio-enhancement effects on human lung adenocarcinoma A549 cells^[1]. 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 µg/mL, respectively^[2]. Amrubicin inhibits the cell cycle profile of U937 cells with an IC₅₀ of 5.6 µM. Amrubicin (20 µM) also induces apoptosis in U937 cells, activates caspase-3/7 and reduces the mitochondrial membrane potential (Δψm)^[3].

In Vivo: Amrubicin (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 (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 alone or combined with tegafur and uracil also suppresses tumor growth in human cancer xenograft models^[2].