Bazedoxifene hydrochloride (Synonyms: TSE-424 hydrochloride)

Cat. No.: HY-A0031A: FAQs
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Bazedoxifene hydrochloride (TSE-424 hydrochloride) is an oral active, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC₅₀s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene hydrochloride can be used for the research of osteoporosis. Bazedoxifene hydrochloride acts as an inhibitor of IL-6/GP130 protein-protein interactions. Bazedoxifene hydrochloride can be used for the research of pancreatic cancer.

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

Bazedoxifene hydrochloride Chemical Structure

CAS No. : 198480-56-7

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Other In-stock Forms of Bazedoxifene hydrochloride:

Bazedoxifene acetate

Other Forms of Bazedoxifene hydrochloride:

Bazedoxifene acetate In-stock
Bazedoxifene Get quote

12 Publications Citing Use of MCE Bazedoxifene hydrochloride

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

IC50: 26 nM (ERα), 99 nM (ERβ)^[1]

In Vitro

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

507.06

Formula

C₃₀H₃₅ClN₂O₃

CAS No.

198480-56-7

SMILES

OC1=CC2=C(N(CC3=CC=C(OCCN4CCCCCC4)C=C3)C(C5=CC=C(O)C=C5)=C2C)C=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

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]

Bazedoxifene hydrochloride Related Classifications

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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	×		=		×
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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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