198481-32-2
198481-32-2 结构式
基本信息
巴多兮芬
巴佐昔芬杂质
巴多昔芬中间体
1-(4-(2-(氮杂环庚烷-1-基)乙氧基)苄基)-2-(4-羟基苯基)-3-甲基-1H-吲哚-5-醇
1-[[4-[2-(氮杂环庚烷-1-基)乙氧基]苯基]甲基]-2-(4-羟基苯基)-3-甲基-吲哚-5-醇
CS-1993
Batoxifene
Bazedoxifen
Bazedoxifene
Bazedoxifeno
Unii-Q16tt9C5bk
BAZEDOXIFENE BASE
Bazedoxifene [inn]
Bazedoxifene free base
物理化学性质
常见问题列表
IC50: 26 nM (ERα), 99 nM (ERβ)
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.
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 (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. |