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Minnelide is a prodrug of triptolide that shows potent antitumor activity in a number of tumor types, particularly in pancreatic cancer. Minnelide causes apoptotic[1].
Minnelide (0-200 nM; 48 hours) shows significantly decreased cell viability in pancreatic cancer cell lines after treatment in the presence, but not in the absence, of phosphatase[2]. Cell Viability Assay[2] Cell Line: Pancreatic cancer cell line: S2-013, MIA PaCa-2, S2-VP10, and Panc-1 cells
Minnelide (injection intraperitoneally; 0.1-0.6 mg/kg; once daily or twice daily) leads to a marked decrease in tumor weight and volume at the end of treatment and increases survival in orthotopic model of pancreatic cancer with MIA PaCa-2-derived human pancreatic tumors[2].Minnelide (injection intraperitoneally; 0.42 mg/kg; once daily; 28 days) prevents locoregional spread and leads to a decrease in average tumor weight in a xenograft model of pancreatic cancer with metastatic S2-013 cells[2].Minnelide (injection intraperitoneally; 0.42 mg/kg, 0.21 mg/kg; once daily) causes tumor regression and tumors from Minnelide-treated animals showed fibrosis and the presence of pyknotic nuclei in human pancreatic cancer xenografts in SCID mice[2]. Animal Model: Orthotopic model of pancreatic cancer with MIA PaCa 2-derived human pancreatic tumors in athymic nude mice[2]
[1]. Noel P，et al. Triptolide and Its Derivatives as Cancer Therapies. Trends Pharmacol Sci. 2019 May;40(5):327-341. [2]. Chugh R, et al. A preclinical evaluation of Minnelide as a therapeutic agent against pancreatic cancer. Sci Transl Med. 2012 Oct 17;4(156):156ra139.
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