Bazedoxifene (Synonyms: TSE-424)

Name: Bazedoxifene
Brand: MedChemExpress
SKU: HY-A0031
Rating: 5.0 (12 reviews)

Cat. No.: HY-A0031 Purity: 99.06%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Bazedoxifene Chemical Structure

CAS No. : 198481-32-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 110	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 110	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 700	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 12 publication(s) in Google Scholar

Other Forms of Bazedoxifene:

12 Publications Citing Use of MCE Bazedoxifene

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 26 nM (ERα), 99 nM (ERβ)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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	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

Molecular Weight

470.60

Formula

C₃₀H₃₄N₂O₃

CAS No.

198481-32-2

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

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Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.06%

Select Batch:

Data Sheet (279 KB) SDS (419 KB)

COA (251 KB) LCMS (92 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Bazedoxifene (Synonyms: TSE-424)

Customer Review

Other Forms of Bazedoxifene:

Bazedoxifene Related Antibodies

12 Publications Citing Use of MCE Bazedoxifene

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Estrogen Receptor/ERR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Bazedoxifene Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Bazedoxifene Related Classifications

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