Bazedoxifene Acetate

Licensed by Pfizer Catalog No.S2167 Synonyms: WAY-140424, TSE-424

Bazedoxifene Acetate Chemical Structure

Molecular Weight(MW): 530.65

Bazedoxifene Acetate is a third generation selective estrogen receptor modulator (SERM).

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1 Customer Review

  • J Med Chem 2014 57(3), 632-41. Bazedoxifene Acetate purchased from Selleck.

Purity & Quality Control

Choose Selective Estrogen/progestogen Receptor Inhibitors

Biological Activity

Description Bazedoxifene Acetate is a third generation selective estrogen receptor modulator (SERM).
Targets
estrogen receptor [1]
Assay
Methods Test Index PMID
Western blot
p-JAK1 / JAK1 / p-JAK2 / JAK2 / Cleaved caspase-3 / Bcl-2 / Survivin ; 

PubMed: 30648776     


Bazedoxifene inhibits signal transducer and activator of transcription (STAT)3 phosphorylation and expression of STAT3 downstream genes, and induces apoptosis. HEPG2 (A), 7721 (B) and HUH‐7 (C) cancer cell lines exhibit constitutively phosphorylated STAT3. Bazedoxifene (10, 15, 20, 25 μmol/L) inhibited the phosphorylation of STAT3 (Tyr 705), Janus kinase (JAK)1 and JAK2, induced apoptosis as evidenced by increased cleaved caspase‐3. The expression of STAT3‐mediated genes was decreased by bazedoxifene except for the expression of Bcl‐2 in 7721 cells. GAPDH, glyceraldehyde 3‐phosphate dehydrogenase.

p-STAT3 / STAT3 / p-AKT / p-ERK / Cleaved Caspase-3 ; 

PubMed: 28672024     


RH30, RD, and RH28 cells were treated with Bazedoxifene at the indicated concentration overnight. The protein expression of interest was determined by Western blot analysis with GAPDH as loading control. 

30648776 28672024
Growth inhibition assay
Cell viability; 

PubMed: 30648776     


HEPG2, HUH‐7 and 7721 liver cancer cells were treated with or without bazedoxifene (5, 10, 15, 20, 30 μmol/L) at 37°C for 24 h. Bazedoxifene inhibited cell viability (*P < 0.05). 

30648776

Protocol

References

Solubility (25°C)

In vitro DMSO 100 mg/mL (188.44 mM)
Ethanol 25 mg/mL warmed (47.11 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 530.65
Formula

C30H34N2O3.C2H4O2

CAS No. 198481-33-3
Storage powder
in solvent
Synonyms WAY-140424, TSE-424

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03475719 Enrolling by invitation Drug: HUG186-B and HUG186-D|Drug: HUG186 Osteoporosis Postmenopausal Huons Co. Ltd. January 11 2018 Phase 1
NCT03005340 Unknown status Drug: Treatment B|Drug: Treatment C|Drug: Treatment BC Healthy Alvogen Korea December 2016 Phase 1
NCT02448771 Active not recruiting Drug: Palbociclib|Drug: Bazedoxifene Breast Cancer Stage IV|Unresectable Locally Advanced Invasive Breast Cancer|Metastatic Invasive Breast Cancer Dana-Farber Cancer Institute|Pfizer July 7 2015 Phase 1|Phase 2
NCT01973738 Unknown status -- Selective Estrogen Receptor Modulator Toshihiko Kono|Tomidahama Hospital January 2012 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Estrogen/progestogen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID