Licensed and Manufactured by Pfizer Catalog No.S2128 Synonyms: TSE-424
Molecular Weight(MW): 507.06
Bazedoxifene HCl is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively.
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Choose Selective Estrogen/progestogen Receptor Inhibitors
|Description||Bazedoxifene HCl is a novel, non-steroidal, indole-based estrogen receptor modulator (SERM) binding to both ERα and ERβ with IC50 of 23 nM and 89 nM, respectively.|
Bazedoxifene is a third generation selective estrogen receptor modulator (SERM). Bazedoxifene does not stimulate ERα mediated transcriptional activity and acts as an antagonist to estradiol in cultured breast cancer (bMCF-7) cells. Similar results are seen in other cell lines including CHO (ovarian), HepG2 (hepatic) or GTI-7 (neuronal) with bazedoxifene having no ERα agonist activity and acting as an antagonist to estradiol action. Bazedoxifene does not stimulate proliferation of MCF-7 cells but did inhibit 17β-estradiol-induced proliferation with IC50 of 0.19 nM. 
|In vivo||In an immature rat model, bazedoxifene increases uterine wet weight 35% at a dose of 0.5 mg/kg compared to an 85% increase with raloxifene at the same dose and a 300% increase in uterine weight with ethinyl estradiol at a dose of 10 μg/kg. Ovarectomized rats treated with 0.3 mg/d bazedoxifene displayed maintenance of bone mass and bone strength similar to effects seen with 2 μg/d ethinyl estradiol, 3 mg/d raloxifene, or sham operated animals. |
Ligand binding competition experiments:Test compounds are initially solubilized in DMSO and the final concentration of DMSO in the binding assay is ≤ 1%. Eight dilutions of each test compound are used as an unlabelled competitor for [3H]17β-estradiol. Typically, a set of compound dilutions would be tested simultaneously on human, rat and mouse ER-α and ER-β. The results are plotted as measured DPM vs. concentration of test compound. For dose-response curve fitting, a four parameter logistic model on the transformed, weighted data are fit and the IC50 is defined as the concentration of compound decreasing maximum [3H]estradiol binding by 50%. For active compounds, the IC50 is determined at least three times. It should be noted that IC50 values are not direct measures of a ligand’s affinity for the receptor. Rather, they can only be compared as relative values, in this case to 17β-estradiol.
|In vitro||DMSO||101 mg/mL (199.18 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02694809||Recruiting||Ductal Breast Carcinoma In Situ|Postmenopausal||Northwestern University|Pfizer|National Cancer Institute (NCI)||January 2017||Phase 2|
|NCT02602704||Recruiting||Arthritis, Rheumatoid||Hanyang University|Pfizer||December 2015||Phase 4|
|NCT02448771||Recruiting||Breast Cancer Stage IV|Unresectable Locally Advanced Invasive Breast Cancer|Metastatic Invasive Breast Cancer||Dana-Farber Cancer Institute|Pfizer||July 2015||Phase 1|Phase 2|
|NCT02090400||Completed||Osteoporosis, Postmenopausal||Instituto Palacios|Pfizer||May 2013||Phase 4|
|NCT01634789||Terminated||Healthy||Pfizer||August 2012||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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