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  3. Bazedoxifene

Bazedoxifene (Synonyms: TSE-424)

Cat. No.: HY-A0031
Handling Instructions

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

Bazedoxifene Chemical Structure

CAS No. : 198481-32-2

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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
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Based on 5 publication(s) in Google Scholar

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Description

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[1][2].

IC50 & Target

IC50: 26 nM (ERα), 99 nM (ERβ)[1]

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].

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].

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.
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)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Bazedoxifene
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HY-A0031
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