Bazedoxifene盐酸巴多昔芬,198480-56-7

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Bazedoxifene hydrochloride

CAS No. : 198480-56-7

MCE 国际站：Bazedoxifene hydrochloride

产品活性：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。

研究领域：Vitamin D Related/Nuclear Receptor

作用靶点：Estrogen Receptor/ERR

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

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

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