Bazedoxifene acetate Estrogen/progestogen Receptor modulator

Cat.No.S2167

Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM).
Bazedoxifene acetate Estrogen/progestogen Receptor modulator Chemical Structure

Chemical Structure

Molecular Weight: 530.65

Quality Control

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 530.65 Formula

C30H34N2O3.C2H4O2

Storage (From the date of receipt)
CAS No. 198481-33-3 -- Storage of Stock Solutions

Synonyms TSE-424, WAY-140424 Smiles CC1=C(N(C2=C1C=C(C=C2)O)CC3=CC=C(C=C3)OCCN4CCCCCC4)C5=CC=C(C=C5)O.CC(=O)O

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (188.44 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 13 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

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.

Mechanism of Action

Targets/IC50/Ki
estrogen receptor [1]

Applications

Methods Biomarkers Images PMID
Western blot p-JAK1 / JAK1 / p-JAK2 / JAK2 / Cleaved caspase-3 / Bcl-2 / Survivin p-STAT3 / STAT3 / p-AKT / p-ERK / Cleaved Caspase-3 S2167-WB1 30648776
Growth inhibition assay Cell viability S2167-viability1 30648776

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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 --

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