Minnelide

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

雷公藤甲素的水溶性前药，对于减少胰腺肿瘤的生长和扩散非常有效。

A water-soluble prodrug of triptolide that is highly effective in reducing pancreatic tumor growth and spread, and improving survival; efficiently downregulates both CD133(-) and CD133(+) population in the tumors, resulting in a 60% decrease in tumor volume; also is very effective as a therapeutic option against Castration Resistant Prostate Cancer (CRPC).Pancreatic Cancer Phase 2.

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. Cell Viability Assay Cell Line:Pancreatic cancer cell line: S2-013, MIA PaCa-2, S2-VP10, and Panc-1 cells Concentration:0.100 nM, 200 nM Incubation Time:48 hours Result:Decreased cell viability of in vitro.

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.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.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. Animal Model:Orthotopic model of pancreatic cancer with MIA PaCa 2-derived human pancreatic tumors in athymic nude mice Dosage:0.1-0.6 mg/kg Administration:Injection intraperitoneally; 0.1-0.6 mg/kg; once daily or twice daily Result:Prevented pancreatic tumor growth in vivo.Animal Model:Xenograft model of pancreatic cancer with metastatic S2-013 cell line in athymic nude mice Dosage:0.42 mg/kg Administration:Injection intraperitoneally; 0.42 mg/kg; once daily Result:Prevented extensive spread from the primary site of injection. Animal Model:Human pancreatic cancer xenograftsin SCID mice Dosage:0.21 mg/kg, 0.42 mg/kg Administration:Injection intraperitoneally; 0.42 mg/kg; once daily Result:Reduced tumor burden in human xenografts from patients.

14-O-phosphonooxymethyltriptolide disodium salt

NF-κB

TAK1

TAK1

Cancer

Pancreatic Cancer

1254702-87-8

514.374

C21H25Na2O10P

>98% (HPLC)

In Vitro:?H2O : 93.33 mg/mL (181.45 mM)

CC(C)C12C(O1)C3C4(O3)C5(CCC6=C(C5CC7C4(C2OCOP(=O)([O-])[O-])O7)COC6=O)C.[Na+].[Na+]

sodium (((5bS,6aS,7aR,8R,8aS,9aS,9bS,10aS,10bS)-8a-isopropyl-10b-methyl-3-oxo-1,2,3,5,5b,6,6a,8,8a,9a,9b,10b-dodecahydrotris(oxireno)[2',3':4b,5;2'',3'':6,7;2''',3''':8a,9]phenanthro[1,2-c]furan-8-yl)oxy)methyl phosphate

(-20℃)

With Ice Pack

≥ 2 years