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Bazedoxifene

Manufactured by Selleck Chemicals
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Bazedoxifene is a selective estrogen receptor modulator (SERM) compound. It acts as an agonist or antagonist on estrogen receptors, depending on the target tissue. Bazedoxifene is primarily used in research applications to study the effects of selective estrogen receptor modulation.

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Lab products found in correlation

Raloxifene, by Bio-Techne (2 mentions) 4 hydroxytamoxifen, by Merck Group (2 mentions) Vinblastine, by Selleck Chemicals (2 mentions) Sorafenib, by Selleck Chemicals (2 mentions) Camptothecin, by Selleck Chemicals (2 mentions) Rapamycin, by Thermo Fisher Scientific (2 mentions) Etoposide, by Thermo Fisher Scientific (2 mentions) Raloxifene, by Selleck Chemicals (2 mentions) Bortezomib, by Thermo Fisher Scientific (2 mentions) Gcn2ib, by MedChemExpress (2 mentions) Jtc 801, by Selleck Chemicals (2 mentions) Ink128, by Selleck Chemicals (2 mentions) D arginine, by Merck Group (2 mentions) Buthionine sulfoximine, by Thermo Fisher Scientific (2 mentions) Bioactive compound library, by Selleck Chemicals (2 mentions) Azd8055, by Selleck Chemicals (2 mentions) L arginine, by Merck Group (2 mentions) L citrulline, by Merck Group (2 mentions) Dimethyl sulfoxide (dmso), by Merck Group (2 mentions) Cycloheximide (chx), by Merck Group (2 mentions)

8 protocols using bazedoxifene

1

Metabolic Modulators for Cell Line Screening

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Ponatinib, Bazedoxifene and Lopinavir were purchased from Selleck Chemicals (Houston, TX, USA). 2-Deoxy-D-glucose (2-DG), O-benzyl-L-Serine (BenSer), 6-diazo-5-oxo-norleucine (DON), bis-2-(5-phenylacetamido-1,2,4-thiadiazol-2-yl)ethyl sulfide (BPTES), Telaglenastat (CB-839), epigallocatechin gallate (EGCG), 2-allyl-1-hydroxy-9,10-anthraquinone (R162), L-buthionine-sulfoximine (BSO), L-glutamine, glutamic acid and dimethyl 2-oxoglutarate were all purchased from Sigma (Sigma-Aldrich, St. Louis, MO, USA). The caspase-3 fluorescence dye was from Sartorius (Sartorius AG, Göttingen, Germany). Human IL-11Rα and negative control siRNA were from Thermofisher Scientific (Scoresby, VIC, Australia).
Stuart S.F., Bezawork-Geleta A., Areeb Z., Gomez J., Tsui V., Zulkifli A., Paradiso L., Jones J., Nguyen H.P., Putoczki T.L., Licciardi P.V., Kannourakis G., Morokoff A.P., Achuthan A.A, & Luwor R.B. (2023). The Interleukin-11/IL-11 Receptor Promotes Glioblastoma Survival and Invasion under Glucose-Starved Conditions through Enhanced Glutaminolysis. International Journal of Molecular Sciences, 24(4), 3356.
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2

Vincristine Cytotoxicity Assay in MB Cells

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Cells were seeded at a density of 105 cells/well in 96-well plates for 16 h to facilitate adhesion, before the addition of vincristine (Sigma, Oakville, ON, Canada) at various concentrations. After 48 h, the fluorometric reagent Cell Titer Blue (Promega, Madison, WI, USA) was added and fluorescence (560Ex/590Em) measured on a spectrophotometer (PE Enspire, Waltham, MA, USA) after 4 h. In some experiments involving microglia co-culture conditioning, MB cells were treated with ruxolitinib, bazedoxifene, or SC144 (Selleckchem, Houston, TX, USA) during the wean-off three day period, prior to replating cells in 96-well plates for combination treatment of the same agent with vincristine. All assays were conducted as three replicates per treatment condition.
Sreenivasan L., Li L.V., Leclair P, & Lim C.J. (2022). Targeting the gp130/STAT3 Axis Attenuates Tumor Microenvironment Mediated Chemoresistance in Group 3 Medulloblastoma Cells. Cells, 11(3), 381.
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3

Comparative Evaluation of Selective ER Modulators

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Fulvestrant (CAS No: 129453–61-8, > 99% purity) was purchased from MedChem Express. Estradiol (E2) (E8875), lasofoxifene (SML1026), 4-hydroxytamoxifen (H7904), and tamoxifen (T5648) were purchased from Sigma. Raloxifene (2280) was purchased from Tocris. GDC-0810 (S7855), bazedoxifene (S2128), and AZD9496 (S8372) were purchased from Selleckchem. GW5638 (5638), GW7604 (7604), and RU 58,668 (RU) were provided by Donald McDonnell (Duke University). G1T48 was provided by G1 Therapeutics, Inc., as analytical grade compound.
Andreano K.J., Wardell S.E., Baker J.G., Desautels T.K., Baldi R., Chao C.A., Heetderks K.A., Bae Y., Xiong R., Tonetti D.A., Gutgesell L.M., Zhao J., Sorrentino J.A., Thompson D.A., Bisi J.E., Strum J.C., Thatcher G.R, & Norris J.D. (2020). G1T48, an oral selective estrogen receptor degrader, and the CDK4/6 inhibitor lerociclib inhibit tumor growth in animal models of endocrine-resistant breast cancer. Breast Cancer Research and Treatment, 180(3), 635-646.
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4

Compound Library Screening for Bioactive Inhibitors

Cited 1 time
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An 1,833-member bioactive compound library, and an independent 86-member PI3K signaling inhibitor library comprising mTOR, PI3K and AKT pathway inhibitors, were obtained from Selleck Chemicals and stored at −80°C. Erastin2, annotated as compound 35MEW28 (Ref.51 (link)) and ML162 were synthesized by Acme Bioscience. Erastin was the kind gift of B. Stockwell (Columbia). Chemical used (supplier) were: DMSO, ferrostatin-1, thapsigargin, tunicamycin, cycloheximide, L-arginine, D-arginine and L-citrulline (Sigma-Aldrich Corporation); bortezomib, rapamycin, etoposide and buthionine sulfoximine (Thermo-Fisher Scientific); INK 128, AZD8055, vinblastine, camptothecin, sorafenib, bazedoxifene, raloxifene and JTC-801 (Selleck Chemicals); and GCN2iB (MedChemExpress). buthionine sulfoximine was dissolved directly into cell media. All other drugs were prepared as stock solutions in DMSO. Stock solutions were stored at −20˚C.
Conlon M., Poltorack C.D., Forcina G.C., Armenta D.A., Mallais M., Perez M.A., Wells A., Kahanu A., Magtanong L., Watts J.L., Pratt D.A, & Dixon S.J. (2021). A Compendium of Kinetic Modulatory Profiles Identifies Ferroptosis Regulators. Nature chemical biology, 17(6), 665-674.
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5

Cell Line Validation Protocol

Cited 2 times
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Fulvestrant (1047) and Raloxifene (2280), were purchased from Tocris. Estradiol (E8875) and 4-hydroxytamoxifen (H7904) were purchased from Sigma. Bazedoxifene (S2128) was purchased from Selleckchem. Lasofoxifene (HYA0038K), RAD1901 (HY19822A), GDC-0810 (HY12864) and AZD9496 (HY12870) were purchased from MedChem Express. SKBR3 and the MCF7 cells used to generate the MCF7I lines were purchased from ATCC which employs STR analysis. MCF7B and T47D cell lines were published previously (32 (link),33 (link)). The McDonnell laboratory routinely completes PCR based Mycoplasma testing on all cell lines. All cell lines were used within 10–15 passages of thawing.
Andreano K.J., Baker J.G., Park S., Safi R., Artham S., Oesterreich S., Jeselsohn R., Brown M., Sammons S., Wardell S.E., Chang C.Y., Norris J.D, & McDonnell D.P. (2020). The dysregulated pharmacology of clinically relevant ESR1 mutants is normalized by ligand-activated WT receptor. Molecular cancer therapeutics, 19(7), 1395-1405.
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6

Compound Library Screening for Bioactive Inhibitors

Cited 1 time
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An 1,833-member bioactive compound library, and an independent 86-member PI3K signaling inhibitor library comprising mTOR, PI3K and AKT pathway inhibitors, were obtained from Selleck Chemicals and stored at −80°C. Erastin2, annotated as compound 35MEW28 (Ref.51 (link)) and ML162 were synthesized by Acme Bioscience. Erastin was the kind gift of B. Stockwell (Columbia). Chemical used (supplier) were: DMSO, ferrostatin-1, thapsigargin, tunicamycin, cycloheximide, L-arginine, D-arginine and L-citrulline (Sigma-Aldrich Corporation); bortezomib, rapamycin, etoposide and buthionine sulfoximine (Thermo-Fisher Scientific); INK 128, AZD8055, vinblastine, camptothecin, sorafenib, bazedoxifene, raloxifene and JTC-801 (Selleck Chemicals); and GCN2iB (MedChemExpress). buthionine sulfoximine was dissolved directly into cell media. All other drugs were prepared as stock solutions in DMSO. Stock solutions were stored at −20˚C.
Conlon M., Poltorack C.D., Forcina G.C., Armenta D.A., Mallais M., Perez M.A., Wells A., Kahanu A., Magtanong L., Watts J.L., Pratt D.A, & Dixon S.J. (2021). A Compendium of Kinetic Modulatory Profiles Identifies Ferroptosis Regulators. Nature chemical biology, 17(6), 665-674.
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7

Evaluating Novel Drug Combinations

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The following drug treatments were used in the study: bazedoxifene (BZA) (Selleck Chem; S212850), 5-fluorouracil (5-FU) (Accord), oxaliplatin (OX) (Accord), SN38 (Selleck Chem; S4908), LCL161 (Selleck Chem; S7009) and Birinapant (Selleck Chem; S7015).
The following cytokine treatments were used in the study: human recombinant IL-6 (Thermo Fisher; BMS341), human recombinant IL-11 (Thermo Fisher; PHC0115) and human recombinant TNF-α (Thermo Fisher; RP75738).
Dmello R.S., Palmieri M., Thilakasiri P.S., Doughty L., Nero T.L., Poh A.R., To S.Q., Lee E.F., Douglas Fairlie W., Mielke L., Parker M.W., Poon I.K., Batlle E., Ernst M, & Chand A.L. (2024). Combination of bazedoxifene with chemotherapy and SMAC-mimetics for the treatment of colorectal cancer. Cell Death & Disease, 15(4), 255.
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8

Estradiol and Bazedoxifene Compound Synthesis

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17β Estradiol, purchased from Sigma Aldrich (St. Louis, MO) was dissolved in DMSO and diluted to various concentrations. Bazedoxifene, purchased from Selleckchem (Houston, TX). EC312, EC313 and EC317 were synthesized in-house at Evestra, Inc. based on structure activity relationship studies.
Nair H.B., Santhamma B., Krishnegowda N.K., Dileep K.V, & Nickisch K.J. (2016). Effects of Combination of Estradiol with Selective Progesterone Receptor Modulators (SPRMs) on Human Breast Cancer Cells In Vitro and In Vivo. PLoS ONE, 11(3), e0151182.
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