Bazedoxifene (WAY-140424) HCl

Licensed and Manufactured by Pfizer Catalog No.S2128 Synonyms: TSE-424

For research use only.

Bazedoxifene HCl (WAY-140424, TSE-424) 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 (WAY-140424) HCl Chemical Structure

CAS No. 198480-56-7

Selleck's Bazedoxifene (WAY-140424) HCl has been cited by 11 Publications

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Biological Activity

Description Bazedoxifene HCl (WAY-140424, TSE-424) 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.
Targets
ERα [1]
(radioligand binding assay)
ERβ [1]
(radioligand binding assay)
23 nM 89 nM
In vitro

Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). Bazedoxifene does not stimulate ERα mediated transcriptional activity and acts as an antagonist to estradiol in cultured breast cancer (bMCF-7) cells. Similar results are seen in other cell lines including CHO (ovarian), HepG2 (hepatic) or GTI-7 (neuronal) with bazedoxifene having no ERα agonist activity and acting as an antagonist to estradiol action.[2] Bazedoxifene does not stimulate proliferation of MCF-7 cells but did inhibit 17β-estradiol-induced proliferation with IC50 of 0.19 nM. [3]

In vivo In an immature rat model, bazedoxifene increases uterine wet weight 35% at a dose of 0.5 mg/kg compared to an 85% increase with raloxifene at the same dose and a 300% increase in uterine weight with ethinyl estradiol at a dose of 10 μg/kg. Ovarectomized rats treated with 0.3 mg/d bazedoxifene displayed maintenance of bone mass and bone strength similar to effects seen with 2 μg/d ethinyl estradiol, 3 mg/d raloxifene, or sham operated animals. [2]

Protocol (from reference)

Kinase Assay:[3]
  • Ligand binding competition experiments:

    Test compounds are initially solubilized in DMSO and the final concentration of DMSO in the binding assay is ≤ 1%. Eight dilutions of each test compound are used as an unlabelled competitor for [3H]17β-estradiol. Typically, a set of compound dilutions would be tested simultaneously on human, rat and mouse ER-α and ER-β. The results are plotted as measured DPM vs. concentration of test compound. For dose-response curve fitting, a four parameter logistic model on the transformed, weighted data are fit and the IC50 is defined as the concentration of compound decreasing maximum [3H]estradiol binding by 50%. For active compounds, the IC50 is determined at least three times. It should be noted that IC50 values are not direct measures of a ligand’s affinity for the receptor. Rather, they can only be compared as relative values, in this case to 17β-estradiol.

Cell Research:[3]
  • Cell lines: MCF-7
  • Concentrations: ~10 nM
  • Incubation Time: 7 days
  • Method: For the proliferation assay, cells are plated at 20,000 cells/well in a 24-well plate in DMEM/F12 (50:50) (phenol red-free) with 10% charcoal/dextran-treated FBS and 1 × GlutaMAX-1. After overnight incubation, the medium is aspirated and treatments in DMEM/F12 (50:50) (phenol red-free) with 2% charcoal/dextran-treated FBS and 1 × GlutaMAX-1 are added to the wells. Each plate has a vehicle (baseline proliferation) and treatments. Treatments included 10 pM 17β-estradiol determined to be the EC80 for 17β-estradiol and 17β-estradiol in combination with six concentrations of BZA. Treatments from d 1 are renewed on d 3 and d 6 by aspirating medium from wells and replacing with fresh medium and treatments. On d 7, cells are detached from the plate using trypsin-EDTA and counted using a Multisizer II.
Animal Research:[2]
  • Animal Models: Sprague Dawley rats
  • Dosages: 0.5 and 5.0 mg/kg
  • Administration: SC

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 507.06
Formula

C30H34N2O3.HCl

CAS No. 198480-56-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(N(C2=C1C=C(C=C2)O)CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=CC=C(C=C5)O.Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03475719 Unknown status 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
NCT01973738 Unknown status -- Selective Estrogen Receptor Modulator Toshihiko Kono|Tomidahama Hospital January 2012 --
NCT00706225 Completed Drug: Bazedoxifene and conjugated estrogens Postmenopause Wyeth is now a wholly owned subsidiary of Pfizer June 2008 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

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