Antitumor agent-80

Antitumor agent-80 (compound 11) is an orally active and potent antitumor agent. Antitumor agent-80 induces apoptosis in tumor cells[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Antitumor agent-80 (compound 11) (5 μM, 48 h) induces apoptosis and increase in PARP cleavage in tumor cells[1]. Antitumor agent-80 (0-10 μM, 96 h) shows cell growth inhibitory activity against breast and hepatocellular carcinoma cell lines[1]. Growth Inhibitory Activity of Antitumor agent-80 against Hepatocellular Carcinoma and Breast Cancer Cell Line Panel[1]. hepatocellular carcinoma IC50 (μM) breast IC50 (μM) Huh7 1.3 MCF7 3.8 HepG2 2.1 MDA-MB231 2.0 SNU475 1.7 MDA-MB468 2.8 Hep3B 3.0 SKBR3 3.5 FOCUS 2.1 ZR75 7.6 Hep40 8.6 MCF10A 12.1 PLC-PRF-5 9.5 Mahlavu 3.2 Western Blot Analysis[1] Cell Line: Huh7, Mahlavu, MDA-MB-231, and MCF-7 cells Concentration: 5 μM Incubation Time: 48 h Result: Caused the increase in PARP cleavage in both breast cancer cells (MCF7 and MDA-MB-231) and hepatocellular carcinoma cells (Mahlavu). Cell Proliferation Assay[1] Cell Line: Huh7, Mahlavu, MDA-MB-231, and MCF-7 cells Concentration: 10 μM, 5 μM, 2.5 μM Incubation Time: 96 h Result: Caused inhibition in the growth of both breast and hepatocellular carcinoma cell lines.

Antitumor agent-80 (compound 11) (40 mg/kg, Orally, twice a week, for 4 weeks) displays antitumor activity in vivo in the Mahlavu hepatocellular carcinoma and the MDA-MB-231 breast cancer xenograft models[1]. Animal Model: Athymic nude mice (6-8 weeks old, with Mahlavu cells or MDA-MB-231 cells)[1] Dosage: 40 mg/kg Administration: Orally, twice a week, for 4 weeks Result: In the Mahlavu xenografts, had a significant reduction (85%) in tumor volume. For MDA-MB-231 xenografts, resulted in about a 50% decrease in tumor volumes as compared to the control group.