Hydroxyflutamide (Synonyms: HFT)

Name: Hydroxyflutamide
Brand: MedChemExpress
SKU: HY-W013272
Rating: 4.5 (1 reviews)

Cat. No.: HY-W013272 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Hydroxyflutamide (HF), an active metabolite of Flutamide, is a potent androgen receptor antagonist (IC₅₀=700 nM). Hydroxyflutamide can be used for the research of prostate cancer.

For research use only. We do not sell to patients.

Hydroxyflutamide Chemical Structure

CAS No. : 52806-53-8

Size	Price	Stock	Quantity
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 290	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Hydroxyflutamide:

Hydroxyflutamide-d6 Get quote
Hydroxyflutamide (Standard) Get quote

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Hydroxyflutamide (HF), an active metabolite of Flutamide, is a potent androgen receptor antagonist (IC₅₀=700 nM). Hydroxyflutamide can be used for the research of prostate cancer^[1]^[2].

IC₅₀ & Target

IC50: 700 nM (androgen receptor)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	25 nM Compound: Hydroxyflutamide	Antagonist activity at androgen receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay Antagonist activity at androgen receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay	[PMID: 19863083]
CWR22R	IC₅₀	0.23 μM Compound: Hydroxyflutamide	Antagonistic activity at AR in human 22Rv1 cells assessed as reduction in cell number by CCK8 assay Antagonistic activity at AR in human 22Rv1 cells assessed as reduction in cell number by CCK8 assay	[PMID: 32847363]
HEK293	IC₅₀	0.3 μM Compound: Hydroxyflutamide	Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of transcriptional activity by luciferase and beta-galactosidase reporter gene assay	[PMID: 23462715]
HeLa	IC₅₀	31 nM Compound: 2, hydroxyflutamide	Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity by reporter gene assay Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity by reporter gene assay	[PMID: 17804229]
HeLa	IC₅₀	31 nM Compound: 2	Antagonist activity at androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone-induced transcriptional activity by reporter gene assay Antagonist activity at androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone-induced transcriptional activity by reporter gene assay	[PMID: 17064916]
NIH3T3	IC₅₀	6.7 x 10^-2 μM Compound: 1b, OH-flu	Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of DHT-induced transcriptional activation after 24 hrs by androgen response element-mediated luciferase reporter gene assay Antagonist activity at human androgen receptor expressed in mouse NIH3T3 cells assessed as inhibition of DHT-induced transcriptional activation after 24 hrs by androgen response element-mediated luciferase reporter gene assay	[PMID: 18707892]
SC-3	IC₅₀	0.35 μM Compound: 5, hydroxyflutamide	Antagonist activity at wild type human recombinant androgen receptor assessed as inhibition of testosterone-induced growth of mouse androgen dependent SC3 cells by WST-1 method Antagonist activity at wild type human recombinant androgen receptor assessed as inhibition of testosterone-induced growth of mouse androgen dependent SC3 cells by WST-1 method	[PMID: 18571420]
SC-3	IC₅₀	0.37 μM Compound: 2	Antagonist activity at androgen receptor in mouse SC3 cells assessed as inhibition of DHT-induced cell growth after 3 days by CCK-8/WST-8 assay Antagonist activity at androgen receptor in mouse SC3 cells assessed as inhibition of DHT-induced cell growth after 3 days by CCK-8/WST-8 assay	[PMID: 24900588]
SC-3	IC₅₀	1.4 μM Compound: Hydroxyflutamide	Antagonist activity at androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell growth after 3 days Antagonist activity at androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell growth after 3 days	[PMID: 23462715]
SC-3	IC₅₀	2.4 x 10^-1 μM Compound: 4	Growth inhibition of mouse SC3 cells after 3 days by WST-8 assay Growth inhibition of mouse SC3 cells after 3 days by WST-8 assay	[PMID: 20521823]

Clinical Trial

Molecular Weight

292.21

Formula

C₁₁H₁₁F₃N₂O₄

CAS No.

52806-53-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C)(O)C(NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (342.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.4222 mL	17.1110 mL	34.2220 mL
5 mM	0.6844 mL	3.4222 mL	6.8444 mL
10 mM	0.3422 mL	1.7111 mL	3.4222 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.56 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (248 KB) HNMR (268 KB) LCMS (266 KB)

Handling Instructions (2659 KB)

References

[1]. Furr BJ, et, al. Casodex: preclinical studies and controversies. Ann N Y Acad Sci. 1995 Jun 12;761:79-96. [Content Brief]

[2]. Liu HL, et, al. A Molecular Modeling Study of the Hydroxyflutamide Resistance Mechanism Induced by Androgen Receptor Mutations. Int J Mol Sci. 2017 Aug 23;18(9):1823. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.4222 mL	17.1110 mL	34.2220 mL	85.5549 mL
	5 mM	0.6844 mL	3.4222 mL	6.8444 mL	17.1110 mL
	10 mM	0.3422 mL	1.7111 mL	3.4222 mL	8.5555 mL
	15 mM	0.2281 mL	1.1407 mL	2.2815 mL	5.7037 mL
	20 mM	0.1711 mL	0.8555 mL	1.7111 mL	4.2777 mL
	25 mM	0.1369 mL	0.6844 mL	1.3689 mL	3.4222 mL
	30 mM	0.1141 mL	0.5704 mL	1.1407 mL	2.8518 mL
	40 mM	0.0856 mL	0.4278 mL	0.8555 mL	2.1389 mL
	50 mM	0.0684 mL	0.3422 mL	0.6844 mL	1.7111 mL
	60 mM	0.0570 mL	0.2852 mL	0.5704 mL	1.4259 mL
	80 mM	0.0428 mL	0.2139 mL	0.4278 mL	1.0694 mL
	100 mM	0.0342 mL	0.1711 mL	0.3422 mL	0.8555 mL

Hydroxyflutamide Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Hydroxyflutamide52806-53-8HFTAndrogen ReceptorFlutamideprostate cancerInhibitorinhibitorinhibit

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Hydroxyflutamide (Synonyms: HFT)

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Other Forms of Hydroxyflutamide:

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Complete Stock Solution Preparation Table

Hydroxyflutamide Related Classifications

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