巴多昔芬
| 中文名称 | 巴多昔芬 |
|---|---|
| 中文同义词 | 巴多昔芬中间体;巴多昔芬;巴佐昔芬杂质;巴多兮芬;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;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;苯卓昔芬;PERFEMIKER]BAZEDOXIFENE,98% |
| 英文名称 | Bazedoxifene |
| 英文同义词 | 1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-indol-5-ol;1-((4-(2-Hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol;1H-Indol-5-ol, 1-((4-(2-(hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-;Bazedoxifene;Bazedoxifene [inn];Bazedoxifeno;Bazedoxifeno [inn-spanish];Tse-424 |
| CAS号 | 198481-32-2 |
| 分子式 | C30H34N2O3 |
| 分子量 | 470.6 |
| EINECS号 | 805-732-1 |
| 相关类别 | 原料药标样;G蛋白偶联受体&G蛋白;医药中间体;中间体;原料药;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;医药原料;生物化工 |
| Mol文件 | 198481-32-2.mol |
| 结构式 |  |
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 |
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-A0031 | Bazedoxifene | 1 mg | 454元 | |
| 2024/01/25 | HY-A0031 | 巴多昔芬 Bazedoxifene | 198481-32-2 | 5mg | 1000元 |