198481-33-3
198481-33-3 結(jié)構(gòu)式
基本信息
醋酸巴多昔芬
醋酸巴澤昔芬
巴多昔芬醋酸鹽
醋酸巴澤多西芬
巴多昔芬乙酸酯
醋酸巴多昔芬 標(biāo)準(zhǔn)品
Way-140424
WAY-TES 424
WAY-TSE-424
Unii-J70472ud3d
3-Oxo Ziprasidone
Bazedoxifene acetat
BAZEDOXIFENE ACETATE
Bazedoxifene acetate [usan]
TSE 424
VIVIANT
WAY-TES 424
物理化學(xué)性質(zhì)
常見問題列表
醋酸巴多昔芬的作用機(jī)制具有獨特之處，是一種新型的選擇性雌激素受體調(diào)節(jié)劑(SERM)，對雌激素受體具有選擇性的調(diào)節(jié)作用。巴多昔芬在身體的某些組織具有雌激素受體激動作用，在人體骨骼具有和雌激素相同的作用(雌激素可延緩骨老化，降低骨折發(fā)生)。
IC50: 26 nM (ERα), 99 nM (ERβ)
Bazedoxifene acetate is a small molecular GP130 inhibitor, which binds to GP130 D1 domain.
Bazedoxifene acetate inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling.
Bazedoxifene acetate (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells.
Bazedoxifene acetate (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells.
Bazedoxifene acetate inhibits STAT3 nuclear translocation induced by IL-6.
Bazedoxifene acetate blocks the cells migration in pancreatic cancer cells by inhibition of GP130.
Western Blot Analysis
| Cell Line: | AsPC-1 cells |
| Concentration: | 10 μM, 20 μM |
| Incubation Time: | 2 hours |
| Result: | Inhibited IL-6, IL-11 or OSM (50 ng/mL) induced STAT3 phosphorylation. |
Apoptosis Analysis
| Cell Line: | Capan-1 cells, BxPC-3 cells, HPAF-II cells, HPAC cells |
| Concentration: | 10 μM, 20 μM (Capan-1); 5 μM, 10 μM (BxPC-3); 10 μM, 20 μM (HPAF-II); 10 μM, 15 μM (HPAC) |
| Incubation Time: | Overnight |
| Result: | Induced apoptosis. |
Bazedoxifene acetate (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. |