Flutamide

Catalog No.S1908 Synonyms: SCH-13521

Flutamide Chemical Structure

Molecular Weight(MW): 276.21

Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.

Size Price Stock Quantity  
In DMSO USD 70 In stock
USD 50 In stock
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2 Customer Reviews

  • Active Stat5a/b increases nuclear levels of antiandrogen-liganded AR in PC-3 cells. PC-3 cells were infected with AdAR, AdPrlR and AdWTStat5a, serum-starved for 12 h, and pretreated with 1 nM DHT, 10 μM Bicalutamide (Bic), 10 μM Flutamide (Flu) or 10 μM MDV3100 (MDV) for 1 h before stimulation with 10 nM Prl for 30 min, where indicated. Immunostaining depicts DAPI, Stat5a/b, AR and merged imaging of Stat5a/b and AR.

    Mol Cancer Ther, 2015, 14(3):713-26. . Flutamide purchased from Selleck.

    Effects of flutamide on Cd-induced Cx43 protein level and cell proliferation. (A) AR and (B) Cx43 were analyzed throughWestern blot. Results are reported as mean ± SD fromthree replicates. (C) Effect of flutamide on Cd-induced cell proliferation at 48 h, determined through an Edu test. *P<0.05 and ** P <0.01 vs. DMSO group; #P< 0.05 and ##P <0.01 vs. DMSO + Cd. AR, androgen receptor; DMSO, dimethyl sulfoxide; NS, no statistical significance.

    J Appl Toxicol, 2017, 37(8):933-942. Flutamide purchased from Selleck.

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Biological Activity

Description Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.
Targets
Androgen Receptor [1]
55 nM(Ki)
In vitro

Flutamide (Eulexin) is an antiandrogen drug. Flutamide-OH, the active metabolite of flutamide, directly binds at rat anterior pituitary androgen receptor with Ki values of 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]

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. [4]

Protocol

Kinase Assay:[1]
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Androgen Receptor Assay:

Aliquots of 100 μl cytosol are incubated at 0-4°C for 18 h with 100 μl of the indicated saturating concentration of [3H]T in the presence or absence of increasing concentrations of nonlabeled T, DHT, flutamide (FLU) or flutamide-OH (FLU-OH). At the end of the incubation, free and bound T are separated by the addition of 200 μl dextran-coated charcoal (1 % charcoal, 0.1% dextran T-70, 0.1% gelatin, 1.5 mM EDTA and 50 mM Tris (pH 7.4)) for 15 min before centrifugation at 2300 × g for another 15 min at 0-4°C. Aliquots (350 μl) of the supernatant are transferred to scintillation vials with 10 ml of an aqueous counting solution before counting in a Beckman LS 330 counter.
Cell Research:[2]
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  • Cell lines: androgen-sensitive Shionogi cell
  • Concentrations: ~1 μM
  • Incubation Time: 40 days
  • Method: Effect of flutamide on the growth of an androgen-sensitive clone (SEM-l) of mouse mammary carcinoma Shionogi cells in culture. The cells are incubated up to 40 days in medium (MEM + 2% dextran-coated charcoal extracted fetal calf serum) containing the compounds at a concentration of 1 μM. Media are changed every second day.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: Male rat
  • Formulation: 1% gelatin-9% NaCl
  • Dosages: 5 mg twice daily, 0.25 ml
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 55 mg/mL (199.12 mM)
Ethanol 55 mg/mL (199.12 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 276.21
Formula

C11H11F3N2O3

CAS No. 13311-84-7
Storage powder
Synonyms SCH-13521

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02918968 Recruiting Prostate Cancer Astellas Pharma Inc|Medivation, Inc. November 2016 Phase 4
NCT02742675 Recruiting Prostate Cancer Fudan University March 2016 Phase 2
NCT02346578 Recruiting Castration-resistant Prostate Cancer Taro Iguchi, MD, PHD|Astellas Pharma Inc|Osaka City University January 2015 --
NCT01889199 Recruiting Polycystic Ovary Syndrome (PCOS) University of California, Los Angeles|University of Wisconsin, Madison|Oregon Health and Science University April 2013 Phase 2
NCT02341404 Completed Prostate Cancer Lidds AB|Uppsala University May 2012 Phase 2
NCT01546987 Active, not recruiting Prostate Cancer Radiation Therapy Oncology Group|National Cancer Institute (NCI)|NRG Oncology May 2012 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID