製品番号: HY-16985

Darolutamide

(別名: ODM-201; BAY-1841788)

9 Cited Publications

カスタマーレビュー

Based on 9 publication(s) in Google Scholar

Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a K_i of 11 nM for rat wild-type AR (wtAR) and IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation. Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation. Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants. Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer.

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純度: 99.49%
CAS 番号: 1297538-32-9
分子式: C₁₉H₁₉ClN₆O₂
分子量:398.85

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Darolutamide 構造式

CAS 番号: 1297538-32-9

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- Parmacokinetics
- 体内実験
- 臨床実験
化学情報
Publications (9)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a K_i of 11 nM for rat wild-type AR (wtAR) and IC₅₀ of 26 nM for human wild-type AR (hAR)-mediated transcriptional activation^[1]. Darolutamide inhibits testosterone-induced AR nuclear translocation and transcriptional activation^[1]. Darolutamide exerts selective effects on AR-positive cells by inhibiting AR-dependent signaling pathways, and its active metabolite retains full antagonistic activity against AR mutants^[1]. Darolutamide can be used for the research of prostate cancer, including androgen receptor-dependent prostate cancer^[1].

IC₅₀ & Target

IC50: 26 nM (AR-HEK293 cells, AR)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	CC₅₀	>50 μM Compound: ODM-201	Antiproliferative activity against African green monkey COS-7 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against African green monkey COS-7 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 38385428]
CWR22R	CC₅₀	>50 μM Compound: ODM-201	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 38385428]
CWR22R	IC₅₀	>30 μM Compound: 1a; ODM-201	Antiproliferative activity against human 22Rv1 expressing AR assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Antiproliferative activity against human 22Rv1 expressing AR assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 31437779]
DU-145	CC₅₀	>50 μM Compound: ODM-201	Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 38385428]
L02	IC₅₀	>30 μM Compound: 1a; ODM-201	Cytotoxicity against human L02 assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Cytotoxicity against human L02 assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 31437779]
LNCaP	CC₅₀	7.04 μM Compound: ODM-201	Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 38385428]
LNCaP	IC₅₀	1.65 μM Compound: 1a; ODM-201	Antiproliferative activity against human LNCAP expressing AR assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Antiproliferative activity against human LNCAP expressing AR assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 31437779]
LNCaP C4-2	CC₅₀	18.75 μM Compound: ODM-201	Antiproliferative activity against human C4-2 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against human C4-2 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 38385428]
PC-3	CC₅₀	>50 μM Compound: ODM-201	Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 38385428]
PC-3	IC₅₀	>30 μM Compound: 1a; ODM-201	Cytotoxicity against human PC3 assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Cytotoxicity against human PC3 assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 31437779]

体外実験

Darolutamide (ODM-201) (0.1 nM-100 μM; 0-4 ℃ overnight) competitively binds to wild-type androgen receptor (wtAR) in cytosolic lysates from rat ventral prostates, with an inhibition constant (Ki) of 11 nM^[1].
Darolutamide (0.1 nM-100 μM; 24 h) inhibits human wild-type AR (hAR)-mediated transcriptional activation in AR-HEK293 cells, with an IC₅₀ of 26 nM^[1].
Darolutamide (0.1 nM-100 μM; 24 h) acts as a full antagonist against mutant ARs (AR(F876L), AR(W741L), AR(T877A)) in transiently transfected U2-OS cells, with IC₅₀ values of 66 nM, 1500 nM, and 1782 nM respectively^[1].
Darolutamide (0.3 μM; 4 h) inhibits testosterone-induced AR nuclear translocation in AR-overexpressing HS-HEK293 cells^[1].
Darolutamide (3 μM; 4 h) inhibits testosterone-induced AR nuclear translocation in AR-overexpressing LN-AR-C cells^[1].
Darolutamide (10 nM-10 μM; 4 days) suppresses androgen-induced cell proliferation in VCaP cells (AR-overexpressing prostate cancer cells). Darolutamide also shows negligible cytotoxicity against AR-negative cells (DU-145 prostate cancer cells, H1581 lung cancer cells)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

VCaP cells (AR-overexpressing prostate cancer cells)
Concentration:

10 nM, 100 nM, 1000 nM, 10000 nM (increasing concentration gradient)
Incubation Time:

4 days
Result:

Suppressed androgen-induced cell proliferation with an IC50 of 230 nM.

Immunofluorescence^[1]

Cell Line:

LNCaP cells
Concentration:

3 μM
Incubation Time:

4 h
Result:

Blocked testosterone-induced AR nuclear translocation.

Immunofluorescence^[1]

Cell Line:

HS-HEK293 cells
Concentration:

0.3 μM, 1 μM
Incubation Time:

4 h (HCS reader), 5 h (confocal imaging)
Result:

Inhibited testosterone-induced nuclear translocation of overexpressed AR.

Parmacokinetics

Species	Dose	Route	AUC_0-∞	C₀	T_1/2	CL	V_d
Mice^[2]	1 mg/kg	i.v.	1343 ng·h/mL	2022 ng/mL	1.74 h	12.4 mL/min/kg	1.87 L/kg

体内実験

Darolutamide (ODM-201) (50 mg/kg; oral administration; once or twice a day; for 37 days) exhibits potent antitumor activity in castrated male BALB/c nude mice bearing subcutaneous VCaP xenografts^[1].
Darolutamide (50 mg/kg; oral administration; twice a day; for 3 weeks) does not increase serum testosterone levels in intact nude mice bearing orthotopic VCaP tumors^[1].
Darolutamide (25, 50, 100 mg/kg; oral administration; twice a day; for 7 days) shows negligible blood-brain barrier penetration with its major active metabolite Ketodarolutamide (HY-19337) having a brain/plasma ratio of 1.9-2.8% in mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male castrated BALB/c nude mice (7 weeks old) were subcutaneously injected with VCaP cells (2 × 10⁶ cells per mouse in 0.1 mL RPMI-1640 medium (HY-K3004) and Matrigel at 1:1 ratio)^[1].
Dosage:

50 mg/kg
Administration:

Oral administration; once or twice daily; for 37 days
Result:

Exhibited potent antitumor activity, with 50 mg/kg twice daily showing more significant efficacy compared to castrated untreated mice.

Animal Model:

Male intact athymic nude mice (7 weeks old) were orthotopically injected with VCaP cells (1 × 10⁶ cells per mouse in 20 μL RPMI-1640 medium) into the dorsal prostate lobes^[1].
Dosage:

50 mg/kg
Administration:

Oral administration; twice daily; for 3 weeks
Result:

Did not increase serum testosterone levels compared to the control group.
Significantly inhibited orthotopic VCaP tumor growth compared to the control group.

Animal Model:

Male nude mice (BALB/c or Balb/cOlaHsd, 8-9 weeks old)^[1].
Dosage:

25, 50, 100 mg/kg
Administration:

Oral administration; twice daily; for 7 days
Result:

Showed negligible blood-brain barrier penetration, with a brain/plasma ratio of 1.9-2.8% across all tested doses, and no dose-response relationship.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1297538-32-9
性状 Solid
分子量 398.85
分子式 C₁₉H₁₉ClN₆O₂
Color White to off-white
SMILES

ClC1=C(C#N)C=CC(C2=NN(C[C@H](C)NC(C3=NNC(C(O)C)=C3)=O)C=C2)=C1
別名

ODM-201; BAY-1841788
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (9)

All Cell Proliferation/Viability Assay2D/3D Cell Culture and DifferentiationWB

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Journal Impact Factor

Cancer Cell

Small-molecule RNA therapeutics to target prostate cancer. [Abstract]

2025 Mar 18:S1535-6108(25)00079-0. PMID: 40118049
NPJ Breast Cancer

Transcriptomic analysis to uncover the mechanism of radiosensitization of AR-positive triple-negative breast cancers with AR inhibition. [Abstract]

2026 Feb 24. PMID: 41735341
Br J Cancer

Androgen and oestrogen receptor co-expression determines the efficacy of hormone receptor-mediated radiosensitisation in breast cancer. [Abstract]

2022 Sep;127(5):927-936. PMID: 35618789

Darolutamide purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2022 Sep;127(5):927-936. [Abstract]

Clonogenic survival assays were performed in AR+/ER+, CAMA-1, ZR-75-1, and BT-474 cells to assess radiosensitization with a one-hour pretreatment of Darolutamide (500 nM, 1 μM, and 2 μM, 1 h) prior to radiation treatment.
Biosensors (Basel)

An Extracellular Matrix Overlay Model for Bioluminescence Microscopy to Measure Single-Cell Heterogeneous Responses to Antiandrogens in Prostate Cancer Cells. [Abstract]

2024 Apr 5;14(4):175. PMID: 38667168

Darolutamide purchased from MedChemExpress. Usage Cited in: Biosensors (Basel). 2024 Apr 5;14(4):175. [Abstract]

IC50 values of three antiandrogen drugs (Apa: apalutamide; Daro: darolutamide; DHT: dihydrotestosterone; Bica: bicalutamide; Enza: enzalutamide, Fluc: Firefly luciferase.) .PCa cell lines (LNCaP, LAPC4, and 22Rv1) were treated with antiandrogen drugs at various concentrations for 120 hours, and cell viability was determined using a colorimetric resazurin assay.
Mol Oncol

TAS3681, an androgen receptor antagonist, prevents drug resistance driven by aberrant androgen receptor signaling in prostate cancer. [Abstract]

2024 Aug;18(8):1980-2000. PMID: 38600681
J Dermatol Sci

Role of androgen signaling in androgen receptor-positive extramammary Paget's disease: Establishment of organoids and their biological analysis as a novel therapeutic target. [Abstract]

2023 Oct;112(1):23-30. PMID: 37661472

Darolutamide purchased from MedChemExpress. Usage Cited in: J Dermatol Sci. 2023 Oct;112(1):23-30. [Abstract]

Darolutamide (5, 10, 20, 50, and 100 nM, 14 days) inhibited cell growth of androgen receptor-positive EMPD organoids after 4 days of pre-culture with 1 nM R1881.

Darolutamide purchased from MedChemExpress. Usage Cited in: J Dermatol Sci. 2023 Oct;112(1):23-30. [Abstract]

Darolutamide (5, 10, 20, 50, and 100 nM, 24 h) decreased the expression levels of FKBP5 and MKI67 in androgen receptor-positive EMPD organoids.
Sci Rep

Drivers of AR indifferent anti-androgen resistance in prostate cancer cells. [Abstract]

2019 Sep 24;9(1):13786. PMID: 31551480

Darolutamide purchased from MedChemExpress. Usage Cited in: Sci Rep. 2019 Sep 24;9(1):13786. [Abstract]

Dose response curves showed the relative proliferation rate at increasing concentrations of the AR inhibitor darolutamide (ODM-201) in LNCaP cells. Measurements were normalized to vehicle-treated cells and set to 100.
bioRxiv

Profiling crystal engineered ligands for targeting treatment resistant androgen receptors. [Abstract]

2026 May 5:2026.05.01.721995. PMID: 42146362
bioRxiv

2026 Mar 18.

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (250.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5072 mL

12.5360 mL

25.0721 mL

5 mM

0.5014 mL

2.5072 mL

5.0144 mL

10 mM

0.2507 mL

1.2536 mL

2.5072 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

モル濃度計算機

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分子量分子量

希釈計算機

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濃度 _(終了) 濃度 _(終了)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.21 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

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参考文献

[1]. Moilanen AM, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms toandrogen signaling-directed prostate cancer therapies. Sci Rep. 2015 Jul 3;5:12007. doi: 10.1038/srep12007. [Content Brief]

[2]. Sulochana SP, et al. Validation of an LC-MS/MS method for simultaneous quantitation of enzalutamide, N-desmethylenzalutamide, apalutamide, darolutamide and ORM-15341 in mice plasma and its application to a mice pharmacokinetic study. J Pharm Biomed Anal. 2018 Jul 15;156:170-180. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5072 mL	12.5360 mL	25.0721 mL	62.6802 mL
	5 mM	0.5014 mL	2.5072 mL	5.0144 mL	12.5360 mL
	10 mM	0.2507 mL	1.2536 mL	2.5072 mL	6.2680 mL
	15 mM	0.1671 mL	0.8357 mL	1.6715 mL	4.1787 mL
	20 mM	0.1254 mL	0.6268 mL	1.2536 mL	3.1340 mL
	25 mM	0.1003 mL	0.5014 mL	1.0029 mL	2.5072 mL
	30 mM	0.0836 mL	0.4179 mL	0.8357 mL	2.0893 mL
	40 mM	0.0627 mL	0.3134 mL	0.6268 mL	1.5670 mL
	50 mM	0.0501 mL	0.2507 mL	0.5014 mL	1.2536 mL
	60 mM	0.0418 mL	0.2089 mL	0.4179 mL	1.0447 mL
	80 mM	0.0313 mL	0.1567 mL	0.3134 mL	0.7835 mL
	100 mM	0.0251 mL	0.1254 mL	0.2507 mL	0.6268 mL

Darolutamide

9 Cited Publications

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Darolutamide

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MedChemExpress（MCE）の使用を引用している文献 Darolutamide

生物活性

化学情報

Publications (9)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Darolutamide

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Lung Cancer Compound Library

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Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

Classic FDA-Approved Drug Library

MedChemExpress（MCE）の使用を引用している文献 Darolutamide

生物活性

化学情報

Publications (9)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Darolutamide 関連分類

HY-16985 関連分類