巴多昔芬
- CAS号:198481-32-2
- 英文名:Bazedoxifene
- 中文名:巴多昔芬
- CBNumber:CB01458163
- 分子式:C30H34N2O3
- 分子量:470.6
- MOL File:198481-32-2.mol
- 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 :Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
- 形态 :Solid
- 酸度系数(pKa) :10.12±0.15(Predicted)
- 颜色 :White to Very Dark Beige
巴多昔芬性质、用途与生产工艺
- 生物活性 Bazedoxifene (TSE-424) 是一种有口服活性的，能透过血脑屏障的，非甾体、选择性的雌激素受体调节剂 (SERM)，对 ERα 和 ERβ 作用的 IC50 值分别为 26 nM 和 99 nM，可用于骨质疏松症的研究。Bazedoxifene 也是一种 IL-6/GP130 蛋白相互作用抑制剂，可用于胰腺癌的研究。
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靶点
IC50: 26 nM (ERα), 99 nM (ERβ)
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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.
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. -
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.
- 更新日期：2024/11/08
- 产品编号：HY-A0031
- 产品名称：Bazedoxifene
- CAS编号：
- 包装：1 mg
- 价格：454元
- 更新日期：2024/11/08
- 产品编号：HY-A0031
- 产品名称：巴多昔芬 Bazedoxifene
- CAS编号：198481-32-2
- 包装：5mg
- 价格：1000元
- 公司名称：TORONTO
- 联系电话：--
- 电子邮件：info@trc-canada.com
- 国家：加拿大
- 产品数：6038
- 优势度：71
