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: 13311-84-7

Selleck's Flutamide has been cited by 17 Publications

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Purity & Quality Control

Batch: Purity: 99.96%
99.96

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Signaling Pathway

Androgen Receptor Signaling Pathways

Androgen Receptor Signaling Pathway

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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
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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