2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. Darolutamide

Darolutamide  (Synonyms: ODM-201; BAY-1841788)

Cat. No.: HY-16985 Purity: 99.49%
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Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a Ki 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.

For research use only. We do not sell to patients.

CAS No. : 1297538-32-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Darolutamide:

Darolutamide Related Antibodies

Top Publications Citing Use of Products

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

    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.

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

    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.

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

    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.

    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.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Darolutamide (ODM-201) is an orally active competitive androgen receptor (AR) antagonist. Darolutamide has a Ki 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]
    In Vitro

    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.

    Darolutamide Related Antibodies

    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 AUC0-∞ C0 T1/2 CL Vd
    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
    In Vivo

    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.
    Clinical Trial
    Molecular Weight

    398.85

    Formula

    C19H19ClN6O2
    CAS No.
    Appearance

    Solid

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5072 mL 12.5360 mL 25.0721 mL
    5 mM 0.5014 mL 2.5072 mL 5.0144 mL
    View the Complete Stock Solution Preparation Table

    * 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

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

    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.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • 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.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
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    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.49%

    SDS (394 KB)

    COA (248 KB) HNMR (271 KB) LCMS (100 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * 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.

    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
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    Darolutamide Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Darolutamide1297538-32-9ODM-201 BAY-1841788ODM201ODM 201BAY1841788BAY 1841788BAY-1841788Androgen Receptorandrogen receptor (AR) competitive antagonistorally activeinhibits AR nuclear translocationinhibits AR transcriptional activationselective for AR-positive cellsfull antagonist against AR mutantsprostate cancerandrogen receptor-dependent prostate cancercastration-resistant prostate cancer (CRPC)VCaP cellsLNCaP cells (LN-AR-C cells)HS-HEK293 cellsU2-OS cellsDU-145 cellsH1581 cellscastrated male BALB/c nude miceintact athymic nude male micemale BalbC miceBalb/cOlaHsd miceInhibitorinhibitorinhibit

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