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Flutamide Androgen Receptor antagonist

Cat.No.S1908

Flutamide (SCH-13521) is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and this compound is primarily used to treat prostate cancer.
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Quality Control

Batch: Purity: 99.96%
99.96

Solubility

In vitro
Batch:

DMSO : 55 mg/mL (199.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 55 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 276.21 Formula

C11H11F3N2O3

Storage (From the date of receipt)
CAS No. 13311-84-7 Download SDF Storage of Stock Solutions

Synonyms SCH-13521 SMILES CC(C)C(=O)NC1=CC(=C(C=C1)[N+](=O)[O-])C(F)(F)F

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
Androgen Receptor
55 nM(Ki)
In vitro
Flutamide (Eulexin) is an antiandrogen drug. Its active metabolite, Flutamide-OH, directly binds at rat anterior pituitary androgen receptor with Ki values of 55 nM. This compound 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. It provides treatment for prostate cancer when used along with leuprolide.
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 this compound (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.
In vivo
Flutamide causes a markedly reduction in rat ventral prostate weight from 319 mg to 245 mg. A combination of this compound and LHRH agonist induces an additive effect with a decrease in prostate weight to 101 mg, and an marked drop in prostatic ODC activity.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/2838689/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-17)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04513717 ACTIVE_NOT_RECRUITING
Prostate Adenocarcinoma; Stage III Prostate Cancer AJCC v8; Stage IVA Prostate Cancer AJCC v8
NRG Oncology
2021-01-21 PHASE3
NCT03678025 RECRUITING
Castration Levels of Testosterone; Metastatic Prostatic Adenocarcinoma; Stage IV Prostate Cancer AJCC v8; Stage IVA Prostate Cancer AJCC v8; Stage IVB Prostate Cancer AJCC v8
SWOG Cancer Research Network
2018-09-24 PHASE3
NCT06694350 NOT_YET_RECRUITING
Head and Neck Squamous Cell Carcinoma
Zhejiang Provincial People's Hospital
2024-12 PHASE2
NCT01786265 ACTIVE_NOT_RECRUITING
Prostate Adenocarcinoma; Recurrent Prostate Carcinoma
M.D. Anderson Cancer Center
2013-02-05 PHASE2
NCT05050084 ACTIVE_NOT_RECRUITING
Prostate Adenocarcinoma
NRG Oncology
2021-12-06 PHASE3
NCT04787744 RECRUITING
Prostate Cancer; Oligometastasis; Oligorecurrence; Recurrent Prostate Cancer; Metastatic Prostate Cancer; De Novo Prostate Cancer
VA Office of Research and Development
2021-07-01 PHASE2; PHASE3

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