Darolutamide (ODM-201)

Synonyms: BAY-1841788

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

Darolutamide (ODM-201) Chemical Structure

CAS: 1297538-32-9

Selleck's Darolutamide (ODM-201) has been cited by 13 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.73%
99.73

Products often used together with Darolutamide (ODM-201)

Apalutamide (ARN-509)


Darolutamide has more potent efficacy on androgen receptors than apalutamide.

Yekeduz E, et al. Prostate Int. 2021 Mar;9(1):1-5.

Enzalutamide


Darolutamide and Enzalutamide are given additionally to castration-resistant PCa (CRPC) patients to fully block the AR-axis.

Ehsani M, et al. Cancers (Basel). 2021 Mar 26;13(7):1534.

Docetaxel


Darolutamide and Docetaxel plus androgen-deprivation therapy increases overall survival in patients with metastatic, hormone-sensitive prostate cancer.

Smith MR, et al. N Engl J Med. 2022 Mar 24;386(12):1132-1142.

Bicalutamide


Darolutamide and Bicalutamide block androgen binding to androgen receptor (AR) and inhibit androgen receptor function.

Michmerhuizen AR, et al. NPJ Breast Cancer. 2020 Sep 25;6:47.

Darolutamide (ODM-201) Related Products

Choose Selective Androgen Receptor Inhibitors

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 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]
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 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.
In Vivo
In vivo In mice bearing VCaP xenografts, ODM-201 (50 mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth. [1]
Animal Research Animal Models BALB/c nude male mice bearing VCaP xenografts
Dosages 50 mg/kg, bid
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04070209 Recruiting
Metastatic Prostate Cancer|Castration-resistant Prostate Cancer
Sir Mortimer B. Davis - Jewish General Hospital
October 19 2020 Phase 2
NCT01317641 Completed
Prostate Cancer
Orion Corporation Orion Pharma|Endo Pharmaceuticals
March 2011 Phase 1|Phase 2

Chemical Information & Solubility

Molecular Weight 398.85 Formula

C19H19ClN6O2

CAS No. 1297538-32-9 SDF Download Darolutamide (ODM-201) SDF
Smiles CC(CN1C=CC(=N1)C2=CC(=C(C=C2)C#N)Cl)NC(=O)C3=NNC(=C3)C(C)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 80 mg/mL ( (200.57 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 38 mg/mL

Water : Insoluble


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In vivo
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