1. Vitamin D Related/Nuclear Receptor
  2. Androgen Receptor
  3. Flutamide

Flutamide is an Androgen Receptor antagonist with Ki=55 nM. Flutamide inhibits prostate cancer progression and has synergistic effects with Docetaxel (HY-B0011). Flutamide also has the potential to protect against hyperthermia-induced multiple organ dysfunction syndrome.

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

CAS No. : 13311-84-7

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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 12 publication(s) in Google Scholar

Other Forms of Flutamide:

Top Publications Citing Use of Products

    Flutamide purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Aug 10:496:139488.  [Abstract]

    Flutamide (2000 μg/L; 28 d) caused widened interstitial spaces and vacuolation in zebrafish testis exposed to PFCAs.

    Flutamide purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Aug 10:496:139488.  [Abstract]

    Flutamide (FT) (2000 μg/L; 28 d) significantly decreased serum T levels and increased E2 and VTG levels in zebrafish.

    Flutamide purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Aug 10:496:139488.  [Abstract]

    Flutamide (FT) (2000 μg/L; 28 d) significantly downregulated androgen synthesis genes and AR pathway related genes (cyp17a1, star, hsd11b2, sox9a, ar and fkbp5) in zebrafish.

    Flutamide purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Aug 10:496:139488.  [Abstract]

    Flutamide (FT) (1 nM-1 μM; 48 h) suppressed proliferation of LNCaP cells dose-dependently.

    Flutamide purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Aug 10:496:139488.  [Abstract]

    Flutamide (FT) (1 nM-1 μM; 24 h) effectively suppressed the transcriptional activity of hAR enhanced by DHT in MDA-kb2 cells.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Flutamide is an Androgen Receptor antagonist with Ki=55 nM. Flutamide inhibits prostate cancer progression and has synergistic effects with Docetaxel (HY-B0011). Flutamide also has the potential to protect against hyperthermia-induced multiple organ dysfunction syndrome[1][2][3][4][5][6][7].

    Cellular Effect
    Cell Line Type Value Description References
    COS-7 IC50
    51.51 μM
    Compound: Flutamide
    Anticancer activity against African green monkey COS7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Anticancer activity against African green monkey COS7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    [PMID: 32866675]
    CV-1 IC50
    110 μM
    Compound: flutamide
    Antagonist activity at human androgen receptor expressed in human CV1 cells assessed as inhibition of receptor-mediated transactivation by MMTV-luciferase reporter gene assay
    Antagonist activity at human androgen receptor expressed in human CV1 cells assessed as inhibition of receptor-mediated transactivation by MMTV-luciferase reporter gene assay
    [PMID: 20826091]
    HCT-15 IC50
    > 100 μM
    Compound: Flutamide
    Anticancer activity against human HCT-15 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Anticancer activity against human HCT-15 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    [PMID: 32866675]
    K562 IC50
    29.2 μM
    Compound: Flutamide
    Anticancer activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Anticancer activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    [PMID: 32866675]
    LNCaP EC50
    7 μM
    Compound: Flutamide
    Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 24 hrs by MTT assay
    10.1039/C6MD00426A
    LNCaP EC50
    7 μM
    Compound: Flutamide
    Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay
    Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay
    [PMID: 28363155]
    LNCaP IC50
    0.9 μM
    Compound: Flutamide
    Anticancer activity against human LNCAP cells after 24 hrs by MTT assay in presence of testosterone
    Anticancer activity against human LNCAP cells after 24 hrs by MTT assay in presence of testosterone
    [PMID: 21600678]
    LNCaP IC50
    11600 nM
    Compound: Flutamide
    Displacement of [3H]R-1881 from Androgen receptor of LNCaP cells
    Displacement of [3H]R-1881 from Androgen receptor of LNCaP cells
    [PMID: 15828836]
    LNCaP IC50
    47.55 μM
    Compound: Flutamide
    Cytotoxicity against human LNCAP cells after 48 hrs by MTT assay
    Cytotoxicity against human LNCAP cells after 48 hrs by MTT assay
    [PMID: 28757062]
    LNCaP IC50
    81.8 μM
    Compound: Flutamide
    Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay
    Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay
    [PMID: 22672984]
    MDA-MB-453 IC50
    2 μM
    Compound: Flutamide
    Antiandrogenic activity in human MDA-MB-453 cells expressing androgen receptor assessed as inhibition of DHT-induced androgen-dependent transcription by luciferase reporter gene assay
    Antiandrogenic activity in human MDA-MB-453 cells expressing androgen receptor assessed as inhibition of DHT-induced androgen-dependent transcription by luciferase reporter gene assay
    [PMID: 19131248]
    NCI-H1299 IC50
    > 500 μM
    Compound: Flutamide
    Anticancer activity against human H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Anticancer activity against human H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 34425478]
    NIH3T3 IC50
    5.8 x 10-7 M
    Compound: 1a, flu
    Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of DHT-induced transcriptional activation after 24 hrs by androgen response element-mediated luciferase reporter gene assay
    Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of DHT-induced transcriptional activation after 24 hrs by androgen response element-mediated luciferase reporter gene assay
    [PMID: 18707892]
    PC-3 IC50
    20.3 μM
    Compound: Flutamide
    Anticancer activity against human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Anticancer activity against human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    [PMID: 32866675]
    PC-3 IC50
    58 μM
    Compound: Flutamide
    Anticancer activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Anticancer activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 34425478]
    PC-3 IC50
    67.34 μM
    Compound: Flutamide
    Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
    Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
    [PMID: 28757062]
    PC-3 IC50
    98.8 μM
    Compound: Flutamide
    Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay
    Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay
    [PMID: 22672984]
    SC-3 IC50
    4.2 μM
    Compound: 4, flutamide
    Antagonist activity at wild type human recombinant androgen receptor assessed as inhibition of testosterone-induced growth of mouse androgen dependent SC3 cells by WST-1 method
    Antagonist activity at wild type human recombinant androgen receptor assessed as inhibition of testosterone-induced growth of mouse androgen dependent SC3 cells by WST-1 method
    [PMID: 18571420]
    SC-3 IC50
    7.2 x 10-7 M
    Compound: 3
    Growth inhibition of mouse SC3 cells after 3 days by WST-8 assay
    Growth inhibition of mouse SC3 cells after 3 days by WST-8 assay
    [PMID: 20521823]
    Sf21 IC50
    143.2 μM
    Compound: Flutamide
    Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    [PMID: 21965623]
    Sf21 IC50
    78.7 μM
    Compound: Flutamide
    Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
    [PMID: 21965623]
    U-251 IC50
    22.11 μM
    Compound: Flutamide
    Anticancer activity against human U-251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    Anticancer activity against human U-251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay
    [PMID: 32866675]
    In Vitro

    The active metabolite of Flutamide, is Flutamide-OH. Both of them directly bind rat anterior pituitary androgen receptor (Ki=55 nM)[1].
    Flutamide does not affect the proliferation of an androgen-sensitive clone of the mouse mammary carcinoma Shionogi SC-l 15 cells in culture, shows only antiandrogenic effect, but not androgenic effect[2].
    Flutamide provides treatment for prostate cancer when used along with Leuprolide[3].
    Flutamide has cytotoxic activity against PC3 and LNCap (IC50s 20 μM and 12 μM, respectively). Flutamide (10 μM, 5 μM; 48 h) induces apoptosis and reduces cell migration and colonization in PC3 and LNCap cells[4].
    Flutamide also downregulates the expression of KLK2 and EMT pathway genes in cells[4].

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

    In Vivo

    Flutamide causes a markedly reduction in rat ventral prostate weight from 319 mg to 245 mg. A combination of Flutamide and LHRH agonist, induces an additive effect with a decrease in prostate weight to 101 mg, and an marked drop in prostatic ODC activity[5].
    Flutamide (12.5-50 mg/kg; sc; once daily for 3 days) alleviates heat stroke in heat-stressed mice[6].

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

    Clinical Trial
    Molecular Weight

    276.21

    Formula

    C11H11F3N2O3

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CC(C)C(NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (362.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.6204 mL 18.1022 mL 36.2043 mL
    5 mM 0.7241 mL 3.6204 mL 7.2409 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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: ≥ 2.5 mg/mL (9.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (9.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    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: 99.94%

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.6204 mL 18.1022 mL 36.2043 mL 90.5108 mL
    5 mM 0.7241 mL 3.6204 mL 7.2409 mL 18.1022 mL
    10 mM 0.3620 mL 1.8102 mL 3.6204 mL 9.0511 mL
    15 mM 0.2414 mL 1.2068 mL 2.4136 mL 6.0341 mL
    20 mM 0.1810 mL 0.9051 mL 1.8102 mL 4.5255 mL
    25 mM 0.1448 mL 0.7241 mL 1.4482 mL 3.6204 mL
    30 mM 0.1207 mL 0.6034 mL 1.2068 mL 3.0170 mL
    40 mM 0.0905 mL 0.4526 mL 0.9051 mL 2.2628 mL
    50 mM 0.0724 mL 0.3620 mL 0.7241 mL 1.8102 mL
    60 mM 0.0603 mL 0.3017 mL 0.6034 mL 1.5085 mL
    80 mM 0.0453 mL 0.2263 mL 0.4526 mL 1.1314 mL
    100 mM 0.0362 mL 0.1810 mL 0.3620 mL 0.9051 mL
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      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.

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    Product Name:
    Flutamide
    Cat. No.:
    HY-B0022
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