Amrubicin (SM-5887) hydrochloride is a DNA topoisomerase II inhibitor that can be utilized in cancer research.

Amrubicin (SM-5887) at a concentration of 2.5 μg/mL demonstrates radio-enhancement effects on human lung adenocarcinoma A549 cells. It inhibits the proliferation of LX-1, A549, A431, and BT-474 cell lines, producing IC50 values of 1.1 ± 0.2, 2.4 ± 0.8, 0.61 ± 0.10, and 3.0 ± 0.3 µg/mL, respectively. Furthermore, Amrubicin (SM-5887) disrupts the cell cycle of U937 cells with an IC50 of 5.6 µM, induces apoptosis, activates caspase-3/7, and decreases the mitochondrial membrane potential (Δψm) at 20 µM.

Administered intravenously at 25 mg/kg, Amrubicin (SM-5887) demonstrates notable antitumor efficacy against SCLC tumors, Lu-24 and Lu-134, achieving T/C values of 17% and 9%, respectively, on day 14. Additionally, Amrubicin combined with cisplatin and irinotecan further inhibits tumor progression compared to the drug alone in mice with LX-1 tumors. Furthermore, Amrubicin (SM-5887), either by itself or in conjunction with tegafur and uracil, effectively reduces tumor growth in human cancer xenograft models.