Flutamide

Catalog No.S1908 Synonyms: SCH-13521

For research use only.

Flutamide (SCH-13521) 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.

Flutamide Chemical Structure

CAS No. 13311-84-7

Selleck's Flutamide has been cited by 15 publications

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Biological Activity

Description Flutamide (SCH-13521) 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 (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[4]
  • Animal Models: Male rat
  • Dosages: 5 mg twice daily, 0.25 ml
  • Administration: s.c.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 276.21
Formula

C11H11F3N2O3

CAS No. 13311-84-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)C(=O)NC1=CC(=C(C=C1)[N+](=O)[O-])C(F)(F)F

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01889199 Recruiting Drug: Flutamide|Other: Placebo Polycystic Ovary Syndrome (PCOS) University of California Los Angeles|Oregon Health and Science University April 2013 Phase 2
NCT02341404 Completed Drug: 2-hydroxyflutamide (2-HOF) Prostate Cancer Lidds AB|Uppsala University May 2012 Phase 2
NCT00006214 Completed Drug: flutamide|Other: placebo Prostate Cancer Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) August 2000 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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