Bazedoxifene hydrochloride(Synonyms: TSE-424 hydrochloride)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Bazedoxifene hydrochloride (Synonyms: TSE-424 hydrochloride)

Bazedoxifene hydrochloride (TSE-424 hydrochloride) 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 hydrochloride 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。

Bazedoxifene hydrochloride(Synonyms: TSE-424 hydrochloride)

Bazedoxifene hydrochloride Chemical Structure

CAS No. : 198480-56-7

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Bazedoxifene hydrochloride 的其他形式现货产品:

Bazedoxifene acetate

生物活性

Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer[1][2].

IC50 & Target

IC50: 26 nM (ERα), 99 nM (ERβ)[1]
体外研究
(In Vitro)

Bazedoxifene hydrochloride is a small molecular GP130 inhibitor, which binds to GP130 D1 domain[1].
Bazedoxifene hydrochloride inhibits STAT3 phosphorylation induced by IL-6 and IL-11 in GP130/STAT3 pathway signaling[1].
Bazedoxifene hydrochloride (10 μM-20 μM; 2 hours) inhibits STAT3 phosphorylation induced by cytokines in human pancreatic cancer cells[2].
Bazedoxifene hydrochloride (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells[2].
Bazedoxifene hydrochloride inhibits STAT3 nuclear translocation induced by IL-6[2].
Bazedoxifene hydrochloride blocks the cells migration in pancreatic cancer cells by inhibition of GP130[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

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[2]

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
(In Vivo)

Bazedoxifene hydrochloride (5 mg/kg; i.g.; daily; for 18 days) inhibits Capan-1 tumor growth in mouse model in vivo[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 6-week-old female athymic nude mice[2]
Dosage: 5 mg/kg
Administration: Oral gavage, daily, for 18 days
Result: Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells.

Clinical Trial

分子量

507.06

Formula

C30H35ClN2O3
CAS 号

198480-56-7
中文名称

盐酸巴多昔芬
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Barry S Komm, et al. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology. 2005 Sep;146(9):3999-4008.

    [2]. Xiaojuan Wu, et al. Bazedoxifene as a Novel GP130 Inhibitor for Pancreatic Cancer Therapy. Mol Cancer Ther. 2016 Nov; 15(11): 2609–2619.

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