Bazedoxifene HCl Licensed and Manufactured by Pfizer

Catalog No.S2128

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.

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Bazedoxifene HCl Chemical Structure

Bazedoxifene HCl Chemical Structure
Molecular Weight: 507.06

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Product Information

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Product Description

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]
IC50 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]
Features

Protocol(Only for 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 Assay: [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 Study: [2]

Animal Models Sprague Dawley rats
Formulation 50% dimethylsulfoxide-50% 1× Dulbecco’s PBS
Dosages 0.5 and 5.0 mg/kg
Administration SC

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Miller CP, et al. J Med Chem, 2001, 44(11), 1654-1657.

[2] Diane M Biskobing, et al. Clin Interv Aging, 2007, 2(3), 299–303.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-06-25)

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  ...more 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

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Chemical Information

Download Bazedoxifene HCl SDF
Molecular Weight (MW) 507.06
Formula

C30H34N2O3.HCl

CAS No. 198480-56-7
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms TSE-424
Solubility (25°C) * In vitro DMSO 101 mg/mL (199.18 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name 1H-Indol-5-ol, 1-[[4-[2-(hexahydro-1H-azepin-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methyl-, hydrochloride (1:1)

Customer Product Validation(1)


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Source J Med Chem 2014 57(3), 632-41. Bazedoxifene HCl purchased from Selleck
Method Western blot
Cell Lines SUM159 cells
Concentrations 10-30 uM
Incubation Time 24 h
Results In human breast cancer cells(SUM159, ER negative) expressing IL-6 and GP130, bazedoxifene (10 − 30 μ M) inhibited the constitutive P-STAT3 activity levels induced by the expressed IL-6 and GP130.

Tech Support

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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