XSJ81 is an orally active anticancer agent. It significantly inhibits the proliferation of ampullary cancer (AC) DPC-X3 cells, with an IC50 of 0.655 μM. XSJ81 suppresses colony formation and arrests the cell cycle at the G2/M phase while inhibiting cell migration. Additionally, XSJ81 induces DNA damage and apoptosis in DPC-X3 cells. In mouse models with DPC-X3 xenograft tumors, XSJ81 exhibits notable antitumor efficacy. This compound is applicable for research on ampullary cancer.

XSJ81 exhibits significant antiproliferative effects on ampullary cancer (AC) DPC-X3 cells with an IC50 of 0.655 μM over 48 hours at concentrations ranging from 0.35 to 40 μM. It reduces EdU fluorescence in DPC-X3 cells in a dose-dependent manner at 0.35-1.4 μM over 48 hours and inhibits colony formation in a dose-dependent way at much lower concentrations (0.003-0.011 μM) over two weeks. XSJ81 also causes G2/M phase arrest, induces apoptosis, and inhibits cell migration in DPC-X3 cells at 0.35-1.4 μM for 24-48 hours. Additionally, XSJ81 triggers dose-dependent γ-H2AX foci formation in the nuclei of DPC-X3 cells at 0.35-1.4 μM within 24 hours. At higher concentrations (200-500 μM), it blocks Topo I-mediated relaxation of supercoiled pBR322 plasmid DNA, maintaining it in a supercoiled state and promoting the proteasomal degradation of the Topo I protein. Furthermore, XSJ81 induces time- and dose-dependent cytotoxicity in adenoid cystic carcinoma organoids (ACOs) at 100-1000 nM over a period of 0-72 hours.

A single oral administration of XSJ81 (100 mg/kg) over 3 to 14 days in 6-week-old female BALB/c mice resulted in no mortality. XSJ81 (5-10 mg/kg), administered intraperitoneally every 48 hours for 14 days, demonstrated significant antitumor activity in nude mice with DPC-X3 xenograft tumors.