MedChemExpress -Model Bazedoxifene acetate -198481-33-3

FromMedChemExpress LLC (MCE)

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

Bazedoxifene acetate

MCE China：Bazedoxifene acetate

Brand：MedChemExpress (MCE)

Cat. No.HY-A0036

CAS：198481-33-3

Synonyms：TSE-424 acetate

Purity：99.98%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.

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

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

IC50 & Target：IC50: 26 nM (ERα), 99 nM (ERβ)[1] In Vitro Bazedoxifene acetate is a small molecular GP130 inhibitor, which binds to GP130 D1 domain[1].?Bazedoxifene acetate inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling[1].?Bazedoxifene acetate (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells[2].?Bazedoxifene acetate (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells[2].?Bazedoxifene acetate inhibits STAT3 nuclear translocation induced by IL-6[2].?Bazedoxifene acetate blocks the cells migration in pancreatic cancer cells by inhibition of GP130[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Bazedoxifene acetate Related Antibodies Western Blot Analysis[2] Cell Line: AsPC-1 cells

References：

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

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

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