ODM-201

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.
Targets
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]

Protocol

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
Formula

C19H19ClN6O2

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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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Androgen Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID