research use only

Flutamide Androgen Receptor antagonist

Name: Flutamide
Brand: Selleck Chemicals
SKU: S1908
Availability: InStock
Rating: 5 (20 reviews)

Cat.No.S1908

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

Chemical Structure

Molecular Weight: 276.21

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.96%

99.96

Related Targets	Adrenergic Receptor Estrogen/progestogen Receptor GPR Glucocorticoid Receptor ACE RAAS Opioid Receptor THR PGES Aromatase 5-alpha Reductase CCK receptor Mineralocorticoid Receptor GHSR SSTR TSH Receptor GNRH Receptor PGDS
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Chemical Information, Storage & Stability

Molecular Weight	276.21	Formula	C₁₁H₁₁F₃N₂O₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	13311-84-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SCH-13521			Smiles	CC(C)C(=O)NC1=CC(=C(C=C1)[N+](=O)[O-])C(F)(F)F

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.750mg/ml (9.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 55 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.350mg/ml (4.89mM)	Taking the 1 mL working solution as an example, add 50 μL of 27 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Androgen Receptor ^[1] 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 K_i values of 55 nM. ^[1] 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. ^[2] It provides treatment for prostate cancer when used along with leuprolide. ^[3]
Kinase Assay	Androgen Receptor Assay
Kinase 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. ^[4]
References	[1] https://pubmed.ncbi.nlm.nih.gov/3956856/ [2] https://pubmed.ncbi.nlm.nih.gov/2462135/ [3] https://pubmed.ncbi.nlm.nih.gov/2503724/ [4] https://pubmed.ncbi.nlm.nih.gov/2838689/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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