Bazedoxifene HCl

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

Bazedoxifene HCl Chemical Structure

Molecular Weight(MW): 507.06

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.

Size Price Stock Quantity  
In DMSO USD 300 In stock
USD 380 In stock

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1 Customer Review

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

Purity & Quality Control

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description 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.
Targets
ERα [1] ERβ [1]
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

Kinase Assay
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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
+ Expand
  • 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.
    (Only for Reference)
Animal Research
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  • Animal Models: Sprague Dawley rats
  • Formulation: 50% dimethylsulfoxide-50% 1× Dulbecco’s PBS
  • Dosages: 0.5 and 5.0 mg/kg
  • Administration: SC
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 101 mg/mL (199.18 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or 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 507.06
Formula

C30H34N2O3.HCl

CAS No. 198480-56-7
Storage powder
in solvent
Synonyms TSE-424

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02694809 Not yet recruiting Ductal Breast Carcinoma In Situ|Postmenopausal Northwestern University|Pfizer|National Cancer Institute (NCI) March 2016 Phase 2
NCT02602704 Not yet recruiting Arthritis, Rheumatoid Hanyang University|Pfizer November 2015 Phase 4
NCT02448771 Recruiting Breast Cancer Stage IV|Unresectable Locally Advanced Invasive Breast Cancer|Metastatic Invasive Breast Cancer Dana-Farber Cancer Institute|Pfizer July 2015 Phase 1|Phase 2
NCT02090400 Completed Osteoporosis, Postmenopausal Instituto Palacios|Pfizer May 2013 Phase 4
NCT01634789 Terminated Healthy Pfizer August 2012 Phase 1
NCT01470326 Active, not recruiting Osteoporosis Pfizer November 2011 --

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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