Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Darolutamide (BAY-1841788) is an androgen receptor (AR) antagonist that blocks AR nuclear translocation (Ki: 11 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 45.00 | |
2 mg | In stock | $ 64.00 | |
5 mg | In stock | $ 107.00 | |
10 mg | In stock | $ 169.00 | |
25 mg | In stock | $ 279.00 | |
50 mg | In stock | $ 397.00 | |
100 mg | In stock | $ 590.00 | |
500 mg | In stock | $ 1,280.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 108.00 |
Description | Darolutamide (BAY-1841788) is an androgen receptor (AR) antagonist that blocks AR nuclear translocation (Ki: 11 nM). |
Targets&IC50 | Androgen receptor:11 nM(Ki) |
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] |
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. |
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) |
Synonyms | ODM-201, BAY-1841788 |
Molecular Weight | 398.85 |
Formula | C19H19ClN6O2 |
CAS No. | 1297538-32-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 74 mg/mL (185.5 mM)
Ethanol: 36 mg/mL (90.3 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
You can also refer to dose conversion for different animals. More
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