Cat. No.: HY-W013272

Hydroxyflutamide

(Synonyms: HFT)

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Based on 1 Customer Validation

Hydroxyflutamide (HFT) is the active metabolite of Flutamide (HY-B0022) and exhibits oral activity. Hydroxyflutamide is a potent androgen receptor antagonist with an IC₅₀ of 700 nM. Hydroxyflutamide can affect embryonic development and reproductive tract development in mice. Additionally, Hydroxyflutamide can enhance the efficacy of Bacillus Calmette-Guérin (BCG) to better inhibit the progression of bladder cancer. Hydroxyflutamide can be used in research related to tumors and reproductive diseases.

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

Purity: 99.77%
CAS No.: 52806-53-8
Formula: C₁₁H₁₁F₃N₂O₄
Molecular Weight:292.21

Storage:

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

Hydroxyflutamide Chemical Structure

CAS No.: 52806-53-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

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

All Akt Isoforms :

All PI3K Isoforms :

All Integrin Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	200 nM Compound: 2	Displacement of [3H]mibolerone from androgen receptor expressed in CHOK1 cells Displacement of [3H]mibolerone from androgen receptor expressed in CHOK1 cells	[PMID: 17064916]
CHO-K1	IC₅₀	200 nM Compound: 2, hydroxyflutamide	Displacement of [3H]mibolerone from human androgen receptor expressed in CHOK1 cells Displacement of [3H]mibolerone from human androgen receptor expressed in CHOK1 cells	[PMID: 17804229]
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]
CV-1	IC₅₀	43 nM Compound: 1b (2-Hydroxyflutamide)	Inhibitory concentration against human androgen receptor (AR) dependent transcriptional activity in co-transfected mammalian CV-1 cells Inhibitory concentration against human androgen receptor (AR) dependent transcriptional activity in co-transfected mammalian CV-1 cells	[PMID: 10743937]
CV-1	IC₅₀	15 nM Compound: 2b	Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells. Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells.	[PMID: 9484511]
CV-1	IC₅₀	2013 nM Compound: 2b	Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells. Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells.	[PMID: 9484511]
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	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]
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]
NIH3T3	IC₅₀	6.7 x 10^-8 M 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]
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	2.4 x 10^-7 M 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]
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]
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	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]
T47D	IC₅₀	45 nM Compound: 54	Antiproliferative activity against human T47D cells Antiproliferative activity against human T47D cells	[PMID: 35786895]

In Vitro

Hydroxyflutamide (0-100 μg/mL; 96 h) exerts a dose-dependent inhibitory effect on the development of mouse 1-cell embryos to the blastocyst stage, with complete inhibition observed at 20 μg/mL^[2].
Hydroxyflutamide (0-100 μg/mL; 72 h) shows a dose-dependent inhibition on blastocyst development in mouse 2-cell embryos. At 20 μg/mL, embryonic development is completely arrested, but this effect can be reversed by Testosterone^[2].
Hydroxyflutamide (5 μM; 0-6 days) can enhance the adhesion/internalization of Bacillus Calmette-Guérin (BCG) in bladder cancer cells (involving the integrin α5β1 pathway), promote the migration of monocytes to BCG-treated bladder cancer cells, and inhibit the proliferation of bladder cancer cells (involving the increased release of TNFα)^[3].
Hydroxyflutamide (100 μM; 0-60 min) inhibits the expression of connexin 43 (a functional marker of Sertoli cells) in primary Sertoli cells isolated from rat testes through activating the PI3K/Akt-dependent pathway^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR^[3]

Cell Line:

Human bladder cancer cell lines T24 and 253J
Concentration:

5 μM
Incubation Time:

Pretreated with 12 h, then co-incubation for 2 h
Result:

Increased the levels of integrin-α5β1.

ELISA Assay^[3]

Cell Line:

THP-1 cells treated BCG
Concentration:

5 μM
Incubation Time:

48 h
Result:

Increased the TNFα production.

In Vivo

Hydroxyflutamide (30 mg; oral gavage; once or twice daily; for two days, on gestational days 15-20) causes hypospadias, prostate agenesis and abnormal seminal vesicle position in male offspring when administered to pregnant FVB/N inbred mice and their male offspring^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 52806-53-8
Appearance Solid
Molecular Weight 292.21
Formula C₁₁H₁₁F₃N₂O₄
Color Light yellow to yellow
SMILES

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

HFT
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 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]. Yallampalli C, et al. Influence of the anti-androgen hydroxyflutamide on in vitro development of mouse embryos. J Reprod Fertil. 1993 Nov;99(2):467-70. [Content Brief]

[3]. Shang Z, et al. Antiandrogen Therapy with Hydroxyflutamide or Androgen Receptor Degradation Enhancer ASC-J9 Enhances BCG Efficacy to Better Suppress Bladder Cancer Progression. Mol Cancer Ther. 2015 Nov;14(11):2586-94. [Content Brief]

[4]. Chojnacka K, et al. Hydroxyflutamide affects connexin 43 via the activation of PI3K/Akt-dependent pathway but has no effect on the crosstalk between PI3K/Akt and ERK1/2 pathways at the Raf-1 kinase level in primary rat Sertoli cells. Toxicol In Vitro. 2016 Mar;31:146-57. [Content Brief]

[5]. Silversides DW, et al. Effects of short-term exposure to hydroxyflutamide in utero on the development of the reproductive tract in male mice. Can J Physiol Pharmacol. 1995 Nov;73(11):1582-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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

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Hydroxyflutamide

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All Akt Isoforms

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Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Hydroxyflutamide Related Classifications

HY-W013272 Related Classifications