| Name | Darolutamide |
| Description | Darolutamide (BAY-1841788) is an androgen receptor (AR) antagonist that blocks AR nuclear translocation (Ki: 11 nM). |
| Cell Research | VCaP cells are treated with a submaximal concentration of mibolerone (0.1?nM) and increasing concentrations of test compounds in steroid-free assay medium supplemented with 4?mM GlutaMAX. After a 4-day incubation with the compounds, cell viability is measured using a WST-1 cell proliferation assay. To rule out non-AR –mediated toxicity, AR-negative PC cells (DU-145) and lung cancer cells (H1581) are treated with an increasing concentration of ODM-201, and cell viability is measured as described above.(Only for Reference) |
| Kinase Assay | AR binding affinity: AR binding affinities of test compounds are studied in cytosolic lysates obtained from ventral prostates of castrated rats by a competition binding assay. Fresh prostates are minced and homogenized with Buffer A containing protease inhibitors. The homogenates are centrifuged and the resultant supernatants are treated with a dextran-coated charcoal solution to remove endogenous steroids. The dissociation constant of the radio ligand [3H]mibolerone for isolated rat ARs is determined in a saturation binding experiment. For the determination of Ki values, prostate cytosol preparations and 1?nM [3H]mibolerone are incubated with increasing concentrations of test compounds overnight. After the incubation, bound and free steroids are separated by treatment with 100?μL of dextran-coated charcoal suspension. Bound radioactivity is determined by counting 100?μL of supernatant fraction in 200?μL of scintillation fluid using a microbeta counter. All procedures are carried out at 0–4?°C. |
| In vitro | In AR-HEK293 cells stably expressing full-length hAR, ODM-201 inhibits human AR (hAR) with IC50 of 26 nM. ODM-201 inhibits VCaP cell proliferation with IC50 of 230 nM, while has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells. [1] |
| In vivo | In mice bearing VCaP xenografts, ODM-201 (50?mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 70 mg/mL (175.5 mM)
Ethanol : 36 mg/mL (90.3 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Inhibitor | Darolutamide | Androgen Receptor | ODM201 | inhibit | BAY1841788 | ODM 201 | BAY 1841788 |
| Inhibitors Related | Dehydroisoandrosterone 3-acetate | Bicalutamide | 2,2,5,7,8-Pentamethyl-6-Chromanol | S-23 | Bavdegalutamide | Enzalutamide | Adrenosterone | Allura Red AC | SK33 | Sunset Yellow FCF | Ostarine | Flutamide |
| Related Compound Libraries | Bioactive Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
