Catalog No.S7559 Synonyms: BAY-1841788

ODM-201 Chemical Structure

Molecular Weight(MW): 398.85

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

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Biological Activity

Description ODM-201 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
  • Formulation: Macrocol + propylene glycol +5% glucose (50:30:20, v/v/v)
  • Dosages: 50 mg/kg, bid
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 80 mg/mL (200.57 mM)
Ethanol 38 mg/mL warmed (95.27 mM)
Water Insoluble

* 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
Synonyms BAY-1841788

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02972060 Not yet recruiting Prostate Cancer European Organisation for Research and Treatment of Cancer - EORTC|Bayer March 2017 Phase 2
NCT03004534 Not yet recruiting Breast Cancer Female Translational Research in Oncology|Bayer February 2017 Early Phase 1
NCT03048110 Not yet recruiting Biological Availability Bayer|Orion Corporation, Orion Pharma February 2017 Phase 1
NCT02933801 Not yet recruiting Prostate Cancer Metastatic|Prostate Cancer Swiss Group for Clinical Cancer Research January 2017 Phase 2
NCT02799602 Recruiting Prostatic Neoplasms Bayer|Orion Corporation, Orion Pharma November 2016 Phase 3
NCT02671097 Completed Healthy Volunteers|Pharmacokinetics|Drug Interaction Bayer February 2016 Phase 1

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Androgen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID