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Darolutamide (ODM-201)

Synonyms: BAY-1841788

Catalog No.S7559 Purity: 99.73%

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

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.

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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 K_i 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
Kinase Assay	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References
[1] Moilanen AM, et al. Sci Rep. 2015, 5:12007. doi: 10.1038/srep12007.

References

[1] Moilanen AM, et al. Sci Rep. 2015, 5:12007. doi: 10.1038/srep12007.

Chemical lnformation & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

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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.

Handling Instructions

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