Darolutamide (ODM-201)

For research use only.

Catalog No.S7559 Synonyms: BAY-1841788

6 publications

Darolutamide (ODM-201) Chemical Structure

CAS No. 1297538-32-9

Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.

Selleck's Darolutamide (ODM-201) has been cited by 6 publications

1 Customer Review

  • Growth suppression effect of different antiandrogens and Chk1 inhibitors on MDA-MB-453 and SUM185PE cells. The effects of a range of concentrations of three antiandrogens (enzalutamide, ENZA; darolutamide, ODM-201; and abiraterone acetate, AA) and two Chk1 inhibitors (GDC-0575 and AZD7762) were assessed by MTT. Histograms represent the respective IC50s (mean of n = 3–4 experiments; error bars show the 95% confidence interval).

    Clin Cancer Res, 2018, doi:10.1158/1078-0432.CCR-18-1469. Darolutamide (ODM-201) purchased from Selleck.

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Biological Activity

Description Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. Phase 3.
Androgen receptor [1]
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:[1]
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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:[1]
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  • Cell lines: DU-145, H1581, and VCaP cells
  • Concentrations: ~10 μM
  • Incubation Time: 4 days
  • Method: 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)
Animal Research:[1]
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  • Animal Models: BALB/c nude male mice bearing VCaP xenografts
  • Dosages: 50 mg/kg, bid
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 80 mg/mL (200.57 mM)
Water Insoluble
Ethanol '38 mg/mL warmed

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 398.85


CAS No. 1297538-32-9
Storage powder
in solvent
Synonyms BAY-1841788
Smiles CC(CN1C=CC(=N1)C2=CC(=C(C=C2)C#N)Cl)NC(=O)C3=NNC(=C3)C(C)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04070209 Recruiting Drug: Darolutamide (BAY1841788)|Radiation: SBRT Metastatic Prostate Cancer|Castration-resistant Prostate Cancer Sir Mortimer B. Davis - Jewish General Hospital October 19 2020 Phase 2
NCT01317641 Completed Drug: ODM-201 Prostate Cancer Orion Corporation Orion Pharma|Endo Pharmaceuticals March 2011 Phase 1|Phase 2

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Androgen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID