Belotecan

Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

IC50: 30 ng/mL (Caski cells), 150 ng/mL (HeLa cells), 150 ng/mL (SiHa cells)[1]

Belotecan (0-600 ng/mL; 0-72 h) time- and dose-dependently inhibits viability of Caski cells, HeLa cells and SiHa cells at 48 h with IC50 values of 30, 150 and 150 ng/mL, respectively[1]. Belotecan (0-150 ng/mL; 48 h) induces cell apoptosis and cell-cycle arrest, and affects PARP, cleaved PARP, BAX, p53, Ser15, cell cycle related protein expression and cancer invasion in cervical cancer[1]. Apoptosis Analysis[1] Cell Line: Caski, HeLa and SiHa cell lines Concentration: 0-150 ng/mL Incubation Time: 48 h Result: Showed strong pro-apoptotic activities to Caski, HeLa and SiHa cells. Western Blot Analysis[1] Cell Line: Caski, HeLa and SiHa cell lines Concentration: 0-150 ng/mL Incubation Time: 48 h Result: Increased the expression of PARP, cleaved PARP, BAX, p53, Ser15, cyclin B1, phosphorylated cyclin B1 and phospho-cdc2 (Tyr15) protein, and decreased MMP2 and VEGF protein expression. Cell Cycle Analysis[1] Cell Line: Caski, HeLa and SiHa cell lines Concentration: 0-150 ng/mL Incubation Time: 48 h Result: Induced cell-cycle arrest in the G2/M phase in cervical cancer. Cell Invasion Assay[1] Cell Line: Caski, HeLa and SiHa cell lines Concentration: 0-150 ng/mL Incubation Time: 48 h Result: Inhibited cancer invasion in cervical cancer.

Belotecan (25 mg/kg; i.v. for 16 days at 4-day intervals) inhibits tumor growth in CaSki-xenografts nude mice[1]. Animal Model: BALB/c-nude mice with CaSki cells injection[1] Dosage: 25 mg/kg Administration: Intravenous injection; 25 mg/kg; 16 days at 4-day intervals Result: Significantly inhibited the tumor growth and showed no significant difference in bodyweight of xenograft mice and the controls.