产品
编 号:F245984
分子式:C30H34N2O3
分子量:470.6
产品类型
结构图
CAS No: 198481-32-2
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产品详情
生物活性:
Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.
体内研究:
Bazedoxifene (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 is a small molecular GP130 inhibitor, which binds to GP130 D1 domain.Bazedoxifene inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling.Bazedoxifene (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells.Bazedoxifene (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells.Bazedoxifene inhibits STAT3 nuclear translocation induced by IL-6.Bazedoxifene blocks the cells migration in pancreatic cancer cells by inhibition of GP130.