Bazedoxifene HCl

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Bazedoxifene HCl 是一种新型非甾体、吲哚类雌激素受体调节剂 (SERM)，与 ERα 和 ERβ 结合，IC50 分别为 23 nM 和 89 nM。

Bazedoxifene HCl is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively.

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. They are for reference only.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 hydrochloride (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 miceDosage:5 mg/kg Administration:Oral gavage, daily, for 18 days Result:Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells.

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Metabolic Enzyme/Protease

P450

ERα| ERβ

Cancer

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198480-56-7

507.06

C30H34N2O3·HCl

>98% (HPLC)

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Cl.CC1=C(N(CC2=CC=C(OCCN3CCCCCC3)C=C2)C2=CC=C(O)C=C12)C1=CC=C(O)C=C1

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(-20℃)

With Ice Pack

≥ 2 years