Darolutamide (ODM-201)

Catalog No.S7559 Synonyms: BAY-1841788

For research use only.

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

Darolutamide (ODM-201) Chemical Structure

CAS No. 1297538-32-9

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

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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.
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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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]
  • 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
Formula

C19H19ClN6O2

CAS No. 1297538-32-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(CN1C=CC(=N1)C2=CC(=C(C=C2)C#N)Cl)NC(=O)C3=NNC(=C3)C(C)O

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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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