Bazedoxifene (WAY-140424) HCl

Synonyms: TSE-424

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

Bazedoxifene (WAY-140424) HCl Chemical Structure

CAS: 198480-56-7

Selleck's Bazedoxifene (WAY-140424) HCl has been cited by 15 Publications

2 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.06%
99.06

Bazedoxifene (WAY-140424) HCl Related Products

Choose Selective Estrogen/progestogen Receptor Inhibitors

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
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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research Animal Models Sprague Dawley rats
Dosages 0.5 and 5.0 mg/kg
Administration SC
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03475719 Unknown status
Osteoporosis Postmenopausal
Huons Co. Ltd.
January 11 2018 Phase 1
NCT03005340 Unknown status
Healthy
Alvogen Korea
December 2016 Phase 1
NCT02729701 Completed
Breast Cancer
University of Kansas Medical Center|Pfizer
May 2016 Phase 2
NCT01973738 Unknown status
Selective Estrogen Receptor Modulator
Toshihiko Kono|Tomidahama Hospital
January 2012 --

Chemical Information & Solubility

Molecular Weight 507.06 Formula

C30H34N2O3.HCl

CAS No. 198480-56-7 SDF --
Smiles CC1=C(N(C2=C1C=C(C=C2)O)CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=CC=C(C=C5)O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (177.49 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Bazedoxifene (WAY-140424) HCl | Bazedoxifene (WAY-140424) HCl ic50 | Bazedoxifene (WAY-140424) HCl price | Bazedoxifene (WAY-140424) HCl cost | Bazedoxifene (WAY-140424) HCl solubility dmso | Bazedoxifene (WAY-140424) HCl purchase | Bazedoxifene (WAY-140424) HCl manufacturer | Bazedoxifene (WAY-140424) HCl research buy | Bazedoxifene (WAY-140424) HCl order | Bazedoxifene (WAY-140424) HCl mouse | Bazedoxifene (WAY-140424) HCl chemical structure | Bazedoxifene (WAY-140424) HCl mw | Bazedoxifene (WAY-140424) HCl molecular weight | Bazedoxifene (WAY-140424) HCl datasheet | Bazedoxifene (WAY-140424) HCl supplier | Bazedoxifene (WAY-140424) HCl in vitro | Bazedoxifene (WAY-140424) HCl cell line | Bazedoxifene (WAY-140424) HCl concentration | Bazedoxifene (WAY-140424) HCl nmr