巴多昔芬

生物活性靶点体外研究体内研究巴多昔芬试剂级价格

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

巴多昔芬化学性质

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 :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。
靶点

IC50: 26 nM (ERα), 99 nM (ERβ)

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.