Home Endocrinology & Hormones Androgen Receptor antagonist Flutamide For research use only.

Flutamide

Synonyms: SCH-13521

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

Flutamide Chemical Structure

CAS No. 13311-84-7

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Flutamide Related Products

Signaling Pathway

Androgen Receptor Signaling Pathways

Androgen Receptor Signaling Pathway

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
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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research Animal Models Male rat
Dosages 5 mg twice daily, 0.25 ml
Administration s.c.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01889199 Completed
Polycystic Ovary Syndrome (PCOS)
University of California Los Angeles|Oregon Health and Science University
 April 2013 Phase 2
NCT02341404 Completed
Prostate Cancer
Lidds AB|Uppsala University
 May 2012 Phase 2
NCT00006214 Completed
Prostate Cancer
Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI)
 August 2000 Phase 2

Chemical Information & Solubility

Molecular Weight 276.21 Formula

C11H11F3N2O3
CAS No. 13311-84-7 SDF Download Flutamide SDF
Smiles CC(C)C(=O)NC1=CC(=C(C=C1)[N+](=O)[O-])C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 55 mg/mL ( (199.12 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 55 mg/mL

Water : Insoluble


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In vivo
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