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Mdv3100

Manufactured by Selleck Chemicals
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MDV3100 is a chemical compound that functions as a selective androgen receptor modulator (SARM). It is primarily used in research laboratories for the study of androgen receptor signaling and its potential applications.

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Lab products found in correlation

Enzalutamide, by Selleck Chemicals (2 mentions) Dimethyl sulfoxide (dmso), by Merck Group (2 mentions) Fetal bovine serum (fbs), by Merck Group (2 mentions) Lncap, by American Type Culture Collection (2 mentions) Du145, by American Type Culture Collection (2 mentions) Lncap, by Selleck Chemicals (1 mentions) Vcap prostate cancer cells, by American Type Culture Collection (1 mentions) R1881, by Selleck Chemicals (1 mentions) Fatty acid, by Merck Group (1 mentions) Insulin, by Thermo Fisher Scientific (1 mentions) Lncap and pc3 cells, by American Type Culture Collection (1 mentions) Tumor necrosis factor (tnf), by R&D Systems (1 mentions) 22rv1 cell, by American Type Culture Collection (1 mentions) Ps 1145, by Merck Group (1 mentions) Ver 155008, by Merck Group (1 mentions) 17 aag, by LC Laboratories (1 mentions) Liposomal clodronate, by Encapsula Nanosciences (1 mentions) Doxorubicin, by Selleck Chemicals (1 mentions) Bez235, by Selleck Chemicals (1 mentions) Flutax 1, by Bio-Techne (1 mentions)

28 protocols using mdv3100

1

Prostate Cancer Cell Line Maintenance and Authentication

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LNCaP (clone FGC), PC-3, and VCaP prostate cancer cells were purchased from American Type Culture Collection. The MR49F cell line was a kind gift from Dr Martin Gleave (Vancouver Prostate Center, Vancouver, BC). All cells were maintained at 37°C in a humidified atmosphere containing 5% CO2. LNCaP and PC-3 cells were cultured in the Roswell Park Memorial Institute-1640 (RPMI-1640) media supplemented with 10% fetal bovine serum (FBS) and VCaP cells were cultured in Dulbecco’s modified Eagle’s medium (DMEM) media supplemented with 10% FBS. The enzalutamide-resistant derivative of the LNCaP cell line, MR49F, was cultured in RPMI-1640 media supplemented with 10% FBS and 10 μM MDV3100.30 (link) MDV3100 was purchased from SelleckChem (S1250; Houston, TX). All cell lines used were authenticated by short tandem repeat analyses at the Johns Hopkins Genetic Resources Core Facility. BMPC-1 cells were as in Markowski et al31 (link) and were cultured in DMEM supplemented with 10% FBS.
BMH-21 was synthesized at the Drug Discovery Division, Lieber Institute (Baltimore, MD), and the chemical structure and purity were verified using liquid chromatography-mass spectrometry and proton nuclear magnetic resonance.
Low J.Y., Sirajuddin P., Moubarek M., Agarwal S., Rege A., Guner G., Liu H., Yang Z., De Marzo A.M., Bieberich C, & Laiho M. (2019). Effective targeting of RNA polymerase I in treatment-resistant prostate cancer. The Prostate, 79(16), 1837-1851.
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2

Prostate Organoids Treated with Enzalutamide

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Prostate organoid cultures were established from Pten(i)pe−/− and Pten/Hif1a(i)pe−/− mice at 3 months AGI and cultured as described (Karthaus et al, 2014 (link); Drost et al, 2016 (link); Abu El Maaty et al, 2022 (link)) and treated for 24 h with enzalutamide (MDV3100; Selleckchem; catalog No.S1250) at 25 and 50 μM, or vehicle (DMSO). C4‐2B (CRL‐3315), DU‐145 (HTB‐81), and PC‐3 (CRL‐1435) cells were obtained from ATCC and cultured in DMEM (4.5 g/l glucose, 10% FCS, 1% penicillin/streptomycin) at 37°C and 5% CO2. Cell lines used were mycoplasma‐free but not recently authenticated. HIF1A silencing in PC‐3 cells was performed as described (Abu El Maaty et al, 2022 (link)).
C4‐2B cells were treated for 24 h with PX‐478 (Selleck Chemicals; catalog No.S7612) at 50 μM and/or with enzalutamide (MDV3100; Selleckchem; catalog No.S1250) at 10, 25 and 50 μM, or vehicle (DMSO). DU‐145 and PC‐3 cells were treated for 24 h with PX‐478 at 50 μM.
Terzic J., Abu el Maaty M.A., Lutzing R., Vincent A., El Bizri R., Jung M., Keime C, & Metzger D. (2023). Hypoxia‐inducible factor 1A inhibition overcomes castration resistance of prostate tumors. EMBO Molecular Medicine, 15(6), e17209.
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3

Prostate and Pancreatic Cancer Cell Lines

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The mouse cell lines, tumorigenic TRAMP-C1, and human prostate cancer cell lines (C4-2, DU145, PC3, and LNCaP) were purchased from the American Type Culture Collection (ATCC; Manassas, VA, USA). All cells were maintained in the culture medium suggested by the ATCC. The mouse pancreatic cell lines (6606PDA, 6606I, and 7265PDA) were kindly provided by Dr. David Tuveson (Cambridge University) via a material transfer agreement. The three pancreatic cancer cell lines were maintained in Dulbecco’s modified Eagle medium/F12 (Invitrogen, Carlsbad, CA, USA) with 10% fetal calf serum, according to established procedures [10 (link)]. In experiments with an AR inhibitor, MDV3100 (Selleckchem, Houston, TX, USA), cells were incubated with 10 µM MDV3100 for 24 h in 10% serum-containing RPMI 1640 medium.
Fan Y.C., Hsu K.C., Lin T.E., Zechner D., Hsu S.P, & Tsai Y.C. (2021). Investigation of Anti-Tumor Effects of an MLK1 Inhibitor in Prostate and Pancreatic Cancers. Biology, 10(8), 742.
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4

Androgen Receptor Modulation Assay

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Assay was performed as previously described (22 ). Briefly, shRNA or pLKO control virus was added to fibronectin-coated (1μg/ml) 96well plates. Cells were plated in RPMI-1640 plus 5%CSS with vehicle, 0-0.05nM R1881, and/or 10μM MDV3100 (Selleck). Quantification was performed on Day 7 using a BioTek Synergy 2 plate reader.
Ta H.Q., Ivey M.L., Frierson HF J.r., Conaway M.R., Dziegielewski J., Larner J.M, & Gioeli D. (2015). Checkpoint kinase 2 (CHK2) negatively regulates androgen sensitivity and prostate cancer cell growth. Cancer research, 75(23), 5093-5105.
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5

Preparation and Administration of Cabazitaxel and MDV3100

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Cabazitaxel (Jevtana©) was generously provided by Sanofi Aventis. For the in vivo administration, Cabazitaxel was prepared by mixing ethanol, polysorbate 80, and 5% (w/v) glucose in sterile water (1:1:18). Solutions were administered intravenously as a slow bolus. CBZ stock (500 μM) was prepared in 100% ethanol and stored at −20°C. MDV3100 was purchased from Selleck Chemicals (Houston, TX). For in vivo administration in mice, MDV3100 was prepared in dimethyl-sulphoxide (DMSO), diluted with sterile PBS (75% PBS: 25% CBZ DMSO Solution) and injected intraperitoneally.
Martin S.K., Pu H., Penticuff J.C., Cao Z., Horbinski C, & Kyprianou N. (2015). Multinucleation and Mesenchymal-to-Epithelial-Transition Alleviate Resistance to Combined Cabazitaxel and Antiandrogen Therapy in Advanced Prostate Cancer. Cancer research, 76(4), 912-926.
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6

Androgen-Resistant Prostate Cancer Cells

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LNCaP-C4-2 cells were purchased from the University of Texas MD Anderson Cancer Center (Houston, TX, USA). Cell lines (22Rv1) were obtained from the University of Colorado Cancer Center (UCCC) Tissue Culture Shared Resource (2014) (Aurora, CO, USA) and were authenticated by Single Tandem Repeat analysis. Cells were passaged in RPMI media containing 10% serum supplemented with amino acids and Insulin (Thermo Fisher, Waltham, MA, USA). MDV3100 or enzalutamide (Selleckchem, Houston, TX, USA) was dissolved as a 20 mM stock in DMSO. Stocks were kept at −20 °C until ready to use. Fatty acids were purchased from Sigma (St. Louis, MO, USA), resuspended in ethanol for a stock solution of 10 mM, and stored at −80 °C. For cell use, Fatty acids were first conjugated to 10% albumin, and then applied to cell media at the indicated concentrations.
Joshi M., Stoykova G.E., Salzmann-Sullivan M., Dzieciatkowska M., Liebman L.N., Deep G, & Schlaepfer I.R. (2019). CPT1A Supports Castration-Resistant Prostate Cancer in Androgen-Deprived Conditions. Cells, 8(10), 1115.
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7

Prostate Cancer Cell Culture and Proliferation Assays

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22Rv1 cells (ATCC) were cultured in RPMI 1640/DMEM (1:1) (Invitrogen) supplemented with 20% FCS and antibiotics (100 U/ml penicillin, 100 μg/ml streptomycin) at 37°C and 5% CO2. LNCaP and PC3 cells (ATCC) were cultured in RPMI 1640 supplemented with 10% FCS and antibiotics. Cells were passaged when they reached 70–80% confluence at 1:5–6 using 0.05% trypsin. For proliferation assays, cells were seeded at a density of 1,000 cells/cm2 in triplicate in 12-well plates and inhibitors or an equal volume of carrier were added the next day. Media were replaced and fresh inhibitors added every other day for 7 days. Cells were then rinsed with PBS, stained with crystal violet, rinsed again, air-dried and images acquired. In some experiments, crystal violet was subsequently solubilized in 10% acetic acid and absorbance measured at 590 nm. The GSK-3 inhibitors CHIR99021 (Axon Medchem and Calbiochem) and BIO-acetoxime (Merck), the IKK inhibitor PS1145 (Sigma) and the AR inhibitor MDV3100 (Selleck Chemicals LLC) were all dissolved in DMSO. TNF (R&D) was dissolved in PBS + 0.1% BSA and DHT (Sigma) in ethanol.
Campa V.M., Baltziskueta E., Bengoa-Vergniory N., Gorroño-Etxebarria I., Wesołowski R., Waxman J, & Kypta R.M. (2014). A screen for transcription factor targets of Glycogen Synthase Kinase-3 highlights an inverse correlation of NFκB and Androgen Receptor Signaling in Prostate Cancer. Oncotarget, 5(18), 8173-8187.
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8

Investigating Molecular Chaperone Inhibitors

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Hsp90 inhibitor 17-AAG (Tanespimycin, see chemical structure in (42 (link))) was purchased from LC Laboratories (Woburn, MA, USA), AR antagonist MDV3100 (Enzalutamide) from Selleck Chemicals. Hsp70 inhibitor VER-155008 (see chemical structure in (43 (link))) was purchased from SIGMA-ALDRICH.. The novel Hsp70 inhibitor UPCMLD18BBQU015254 (18BBQU) was synthesized as previously reported (44 (link)–46 (link)).
Dong J., Wu Z., Wang D., Pascal L.E., Nelson J.B., Wipf P, & Wang Z. (2018). Hsp70 binds to the androgen receptor N-terminal domain and modulates the receptor function in prostate cancer cells. Molecular cancer therapeutics, 18(1), 39-50.
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9

Nanoparticle Formulation Characterization

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Dextran (MW: 10 000, 100 000 and 450 000–650 000), gadolinium acetate, and DMSO were obtained from Sigma-Aldrich (St Louis, MO). The fluorophores DiI and DiR were purchased from Life Technologies (Carlsbad, CA), Flutax1 from Tocris Bioscience (Minneapolis, MN), whereas Doxorubicin, AZD6244, BEZ235, and MDV3100 from Selleck Chemicals (Houston, TX). The clodrosomes (liposomal clodronate) were bought from Encapsula NanoSciences, LLC (Brentwood, TN).
Kaittanis C., Shaffer T.M., Bolaender A., Appelbaum Z., Appelbaum J., Chiosis G, & Grimm J. (2015). Multifunctional MRI/PET Nanobeacons Derived from the in Situ Self-Assembly of Translational Polymers and Clinical Cargo through Coalescent Intermolecular Forces. Nano letters, 15(12), 8032-8043.
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10

Extraction and Preparation of Medicinal Mushroom Compound

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WBM extract was prepared via hot water extraction. Briefly, 6 g of freeze-dried WBM powder generated from 60 g fresh mushrooms were boiled in 1 L hot water for 3 h. The broth was centrifuged at 3000 × g for 30 min, twice, to collect the fraction of the supernatant. The liquid fraction was rotor-evaporated to dryness and then re-dissolved in 1 mL of hot water to produce a 6× mushroom extract (6 mg/µL)3 (link). Enza, an AR antagonist, was purchased from Selleckchem (MDV3100, Selleckchem, Houston, TX). LT, a shiitake mushroom-derived immunomodulatory β-(1, 3)-glucan, was purchased from Carbosynth (FL33321, Compton, Berkshire, UK).
Wang X., Ha D., Yoshitake R, & Chen S. (2021). White button mushroom interrupts tissue AR-mediated TMPRSS2 expression and attenuates pro-inflammatory cytokines in C57BL/6 mice. NPJ Science of Food, 5, 20.
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