巴多昔芬
巴多昔芬 性质
| 熔点 | 98-102° |
|---|---|
| 沸点 | 694.4±55.0 °C(Predicted) |
| 密度 | 1.19 |
| 储存条件 | Sealed in dry,Store in freezer, under -20°C |
| 溶解度 | 可溶于氯仿（少许）、DMSO（少许）、甲醇（少许） |
| 形态 | 固体 |
| 酸度系数(pKa) | 10.12±0.15(Predicted) |
| 颜色 | 白色至深米色 |
巴多昔芬 用途与合成方法
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. |
巴多昔芬 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-A0031 | 1 mg | 454 | ||
| 2024-11-08 | HY-A0031 | 巴多昔芬 | 198481-32-2 | 5mg | 1000 |
