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编 号:F597511
分子式:C30H35ClN2O3
分子量:507.06
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生物活性:
Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer.

体内研究:
Bazedoxifene hydrochloride (5 mg/kg; i.g.; daily; for 18 days) inhibits Capan-1 tumor growth in mouse model in vivo.Animal Model:6-week-old female athymic nude mice
Dosage:5 mg/kg
Administration:Oral gavage, daily, for 18 days
Result:Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells.

体外研究:
Bazedoxifene hydrochloride is a small molecular GP130 inhibitor, which binds to GP130 D1 domain.Bazedoxifene hydrochloride inhibits STAT3 phosphorylation induced by IL-6 and IL-11 in GP130/STAT3 pathway signaling.Bazedoxifene hydrochloride (10 μM-20 μM; 2 hours) inhibits STAT3 phosphorylation induced by cytokines in human pancreatic cancer cells.Bazedoxifene hydrochloride (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells.Bazedoxifene hydrochloride inhibits STAT3 nuclear translocation induced by IL-6.Bazedoxifene hydrochloride blocks the cells migration in pancreatic cancer cells by inhibition of GP130.
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