Art. -Nr.: HY-A0031

Bazedoxifene

(Synonyms: TSE-424)

17 Cited Publications

Kundenbewertung

Based on 17 publication(s) in Google Scholar

Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC₅₀s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer.

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Reinheit: 99.06%
CAS. Nr.: 198481-32-2
Formel: C₃₀H₃₄N₂O₃
Molecular Weight:470.60

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Bazedoxifene Chemical Structure

CAS. Nr.: 198481-32-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (17)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 26 nM (ERα), 99 nM (ERβ)^[1]

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	38.48 μM Compound: Baz	Cytotoxicity against human HEK293 cells incubated for 48 hrs by MTT assay Cytotoxicity against human HEK293 cells incubated for 48 hrs by MTT assay	[PMID: 38665833]
HeLa	IC₅₀	3.43 μM Compound: Bazedoxifene	Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay	[PMID: 29624387]
MCF7	IC₅₀	0.4 nM Compound: 3	Antiproliferative activity against human breast cancer MCF7 cell line in presence of 0.003 nM estradiol Antiproliferative activity against human breast cancer MCF7 cell line in presence of 0.003 nM estradiol	[PMID: 16203138]
MCF7	IC₅₀	3.7 nM Compound: 7 ; TSE-424	In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiol In vitro antagonist effect on estrogen receptor alpha transcriptional activation in MCF-7 cells against 10 pM 17-beta-estradiol	[PMID: 11356100]
MCF7	IC₅₀	7.31 μM Compound: Baz	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 38665833]
MDA-MB-231	IC₅₀	6.73 μM Compound: Baz	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 38665833]
MDA-MB-231	IC₅₀	7.45 μM Compound: 60; TSE-424	Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Anticancer activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 33650861]
MDA-MB-468	IC₅₀	3.14 μM Compound: 60; TSE-424	Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 33650861]
MH60	IC₅₀	3.8 μM Compound: 2	Cytotoxicity in mouse MH60 cells assessed as inhibition of recombinant human IL-6-induced growth incubated for 72 hrs by tetrazolium method Cytotoxicity in mouse MH60 cells assessed as inhibition of recombinant human IL-6-induced growth incubated for 72 hrs by tetrazolium method	[PMID: 36971365]
MIA PaCa-2	IC₅₀	9.7 μM Compound: Bazedoxifene	Cytotoxicity against human MIAPaCa2 cells assessed as cell viability Cytotoxicity against human MIAPaCa2 cells assessed as cell viability	[PMID: 24456369]
SUM-159-PT	IC₅₀	24.9 μM Compound: Bazedoxifene	Cytotoxicity against ER-negative human SUM159 cells assessed as cell viability after 72 hrs by MTT assay in presence of IL-6 Cytotoxicity against ER-negative human SUM159 cells assessed as cell viability after 72 hrs by MTT assay in presence of IL-6	[PMID: 24456369]
T47D	IC₅₀	14.23 μM Compound: Baz	Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Antiproliferative activity against human T47D cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 38665833]
T47D	IC₅₀	16.43 μM Compound: Bazedoxifene	Antiproliferative activity against human T47D cells after 48 hrs by MTT assay Antiproliferative activity against human T47D cells after 48 hrs by MTT assay	[PMID: 29198894]
Vero	CC₅₀	14.97 μM Compound: Bazedoxifene	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	3.44 μM Compound: Bazedoxifene	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730

In Vitro

Bazedoxifene is a small molecular GP130 inhibitor, which binds to GP130 D1 domain^[1].
Bazedoxifene inhibits STAT3 phosphorylation induced by Il-6 and IL-11 in GP130/STAT3 pathway signaling^[1].
Bazedoxifene (10 μM-20 μM; 2 hours) inhibits STAT3 Phosphorylation Induced by cytokines in human pancreatic cancer cells^[2].
Bazedoxifene (5-20 μM; overnight) induces apoptosis in human pancreatic cancer cells^[2].
Bazedoxifene inhibits STAT3 nuclear translocation induced by IL-6^[2].
Bazedoxifene blocks the cells migration in pancreatic cancer cells by inhibition of GP130^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[2]

Cell Line:

AsPC-1 cells
Concentration:

10 μM, 20 μM
Incubation Time:

2 hours
Result:

Inhibited IL-6, IL-11 or OSM (50 ng/mL) induced STAT3 phosphorylation.

Apoptosis Analysis^[2]

Cell Line:

Capan-1 cells, BxPC-3 cells, HPAF-II cells, HPAC cells
Concentration:

10 μM, 20 μM (Capan-1); 5 μM, 10 μM (BxPC-3); 10 μM, 20 μM (HPAF-II); 10 μM, 15 μM (HPAC)
Incubation Time:

Overnight
Result:

Induced apoptosis.

In Vivo

Bazedoxifene (5 mg/kg; i.g.; daily, for 18 days) inhibits Capan-1 tumor growth in mouse model in vivo^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

6-week-old female athymic nude mice^[2]
Dosage:

5 mg/kg
Administration:

Oral gavage, daily, for 18 days
Result:

Suppressed pancreatic cancer xenograft tumor growth and induced apoptosis in tumor cells.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 198481-32-2
Appearance Solid
Molecular Weight 470.60
Formel C₃₀H₃₄N₂O₃
Color White to yellow
SMILES

CC1=C(C2=CC=C(O)C=C2)N(CC3=CC=C(OCCN4CCCCCC4)C=C3)C5=CC=C(O)C=C51
Synonyms

TSE-424
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (17)

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Journal Impact Factor

Nat Commun

Mitochondrial vulnerability underlies myocarditis from COVID-19 mRNA vaccine. [Abstract]

2026 Apr 1;17(1):4716. PMID: 41922346
Free Radic Biol Med

IL-6/gp130/STAT3 signaling contributed to the activation of the PERK arm of the unfolded protein response in response to chronic β-adrenergic stimulation. [Abstract]

2023 Aug 20:205:163-174. PMID: 37307935
J Med Chem

Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. [Abstract]

2020 Oct 8;63(19):11085-11099. PMID: 32886512
Glia

Remyelination in neuromyelitis optica spectrum disorder is promoted by edaravone through mTORC1 signaling activation. [Abstract]

2023 Feb;71(2):284-304. PMID: 36089914
Eur J Pharmacol

Bazedoxifene attenuates intestinal injury in sepsis by suppressing the NF-κB/NLRP3 signaling pathways. [Abstract]

2023 May 15:947:175681. PMID: 36965746
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
iScience

Bazedoxifene rescues hepatocytes from chemically induced oxidative ferroptotic injury in vivo and in vitro by inhibiting protein disulfide isomerase. [Abstract]

2026 Feb 6;29(3):114931. PMID: 41782827
Gynecol Oncol

Constitutively active ESR1 mutations in gynecologic malignancies and clinical response to estrogen-receptor directed therapies. [Abstract]

2019 Jul;154(1):199-206. PMID: 30987772
Sci Rep

Novel soluble bazedoxifene formulation gains antiproliferative and migrastatic effect in squamous cell carcinoma cells. [Abstract]

2026 Mar 17. PMID: 41844825
mSphere

Bazedoxifene Suppresses Intracellular Mycobacterium tuberculosis Growth by Enhancing Autophagy. [Abstract]

2020 Apr 8;5(2):e00124-20. PMID: 32269154
Arch Biochem Biophys

Role of protein disulfide isomerase in mediating sulfasalazine-induced ferroptosis in HT22 cells: The PDI-NOS-NO-ROS/lipid-ROS cascade. [Abstract]

2025 Jun:768:110366. PMID: 40023379
Breast Cancer Res Treat

Pharmacokinetic and pharmacodynamic analysis of fulvestrant in preclinical models of breast cancer to assess the importance of its estrogen receptor-α degrader activity in antitumor efficacy. [Abstract]

2020 Jan;179(1):67-77. PMID: 31562570
J Cell Biochem

Novel chemical scaffold as potential drug against Leishmania donovani: Integrated computational and experimental approaches. [Abstract]

2023 Sep;124(9):1404-1422. PMID: 37566640
University of Colorado Denver

2024.
biorxiv

2024 May 21.
Research Square Preprint

2022 Jul.
Res Sq

Sex differences in viral entry protein expression, host responses to SARS-CoV-2, and in vitro responses to sex steroid hormone treatment in COVID-19. [Abstract]

2020 Dec 31:rs.3.rs-100914. PMID: 33173861

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (212.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1249 mL

10.6247 mL

21.2495 mL

5 mM

0.4250 mL

2.1249 mL

4.2499 mL

10 mM

0.2125 mL

1.0625 mL

2.1249 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.31 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
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- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Barry S Komm, et al. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology. 2005 Sep;146(9):3999-4008. [Content Brief]

[2]. Xiaojuan Wu, et al. Bazedoxifene as a Novel GP130 Inhibitor for Pancreatic Cancer Therapy. Mol Cancer Ther. 2016 Nov; 15(11): 2609–2619. [Content Brief]

[3]. R.A. Hill, et al. Bazedoxifene – a promising brain active SERM that crosses the blood brain barrier and enhances spatial memor. Psychoneuroendocrinology. Volume 121, November 2020, 104830 [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1249 mL	10.6247 mL	21.2495 mL	53.1237 mL
	5 mM	0.4250 mL	2.1249 mL	4.2499 mL	10.6247 mL
	10 mM	0.2125 mL	1.0625 mL	2.1249 mL	5.3124 mL
	15 mM	0.1417 mL	0.7083 mL	1.4166 mL	3.5416 mL
	20 mM	0.1062 mL	0.5312 mL	1.0625 mL	2.6562 mL
	25 mM	0.0850 mL	0.4250 mL	0.8500 mL	2.1249 mL
	30 mM	0.0708 mL	0.3542 mL	0.7083 mL	1.7708 mL
	40 mM	0.0531 mL	0.2656 mL	0.5312 mL	1.3281 mL
	50 mM	0.0425 mL	0.2125 mL	0.4250 mL	1.0625 mL
	60 mM	0.0354 mL	0.1771 mL	0.3542 mL	0.8854 mL
	80 mM	0.0266 mL	0.1328 mL	0.2656 mL	0.6640 mL
	100 mM	0.0212 mL	0.1062 mL	0.2125 mL	0.5312 mL

Bazedoxifene

17 Cited Publications

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Bazedoxifene

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Publications Citing Use of MedChemExpress (MCE) Bazedoxifene

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bazedoxifene

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Pancreatic Cancer Compound Library

Rare Diseases Drug Library

Antidepressant Compound Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Pain-Related Compound Library

Withdrawn Drug Compound Library

Off-patent Drug Library

Membrane Receptor-targeted Compound Library

Mitochondrial Toxicity Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Bazedoxifene

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (17)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bazedoxifene Related Classifications

Art. -Nr.: HY-A0031