Cat. No.: HY-B0022

Flutamide

(Synonyms: SCH 13521)

12 Cited Publications

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Based on 12 publication(s) in Google Scholar

Flutamide is an Androgen Receptor antagonist with Ki=55 nM. Flutamide inhibits prostate cancer progression and has synergistic effects with Docetaxel (HY-B0011). Flutamide also has the potential to protect against hyperthermia-induced multiple organ dysfunction syndrome.

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Pureté: 99.94%
CAS No.: 13311-84-7
Formule: C₁₁H₁₁F₃N₂O₃
Masse moléculaire:276.21

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Flutamide Chemical Structure

CAS No.: 13311-84-7

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (12)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
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Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	51.51 μM Compound: Flutamide	Anticancer activity against African green monkey COS7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Anticancer activity against African green monkey COS7 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 32866675]
CV-1	IC₅₀	110 μM Compound: flutamide	Antagonist activity at human androgen receptor expressed in human CV1 cells assessed as inhibition of receptor-mediated transactivation by MMTV-luciferase reporter gene assay Antagonist activity at human androgen receptor expressed in human CV1 cells assessed as inhibition of receptor-mediated transactivation by MMTV-luciferase reporter gene assay	[PMID: 20826091]
HCT-15	IC₅₀	>100 μM Compound: Flutamide	Anticancer activity against human HCT-15 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Anticancer activity against human HCT-15 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 32866675]
K562	IC₅₀	29.2 μM Compound: Flutamide	Anticancer activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Anticancer activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 32866675]
LNCaP	IC₅₀	11600 nM Compound: Flutamide	Displacement of [3H]R-1881 from Androgen receptor of LNCaP cells Displacement of [3H]R-1881 from Androgen receptor of LNCaP cells	[PMID: 15828836]
LNCaP	IC₅₀	0.9 μM Compound: Flutamide	Anticancer activity against human LNCAP cells after 24 hrs by MTT assay in presence of testosterone Anticancer activity against human LNCAP cells after 24 hrs by MTT assay in presence of testosterone	[PMID: 21600678]
LNCaP	IC₅₀	81.8 μM Compound: Flutamide	Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay	[PMID: 22672984]
LNCaP	EC₅₀	7 μM Compound: Flutamide	Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay	[PMID: 28363155]
LNCaP	IC₅₀	47.55 μM Compound: Flutamide	Cytotoxicity against human LNCAP cells after 48 hrs by MTT assay Cytotoxicity against human LNCAP cells after 48 hrs by MTT assay	[PMID: 28757062]
LNCaP	EC₅₀	7 μM Compound: Flutamide	Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 24 hrs by MTT assay	10.1039/C6MD00426A
MDA-MB-453	IC₅₀	2 μM Compound: Flutamide	Antiandrogenic activity in human MDA-MB-453 cells expressing androgen receptor assessed as inhibition of DHT-induced androgen-dependent transcription by luciferase reporter gene assay Antiandrogenic activity in human MDA-MB-453 cells expressing androgen receptor assessed as inhibition of DHT-induced androgen-dependent transcription by luciferase reporter gene assay	[PMID: 19131248]
NCI-H1299	IC₅₀	>500 μM Compound: Flutamide	Anticancer activity against human H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Anticancer activity against human H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34425478]
NIH3T3	IC₅₀	5.8 x 10^-7 M Compound: 1a, 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	5.8 x 10^-1 μM Compound: 1a, 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]
PC-3	IC₅₀	98.8 μM Compound: Flutamide	Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay	[PMID: 22672984]
PC-3	IC₅₀	67.34 μM Compound: Flutamide	Cytotoxicity against human PC3 cells after 48 hrs by MTT assay Cytotoxicity against human PC3 cells after 48 hrs by MTT assay	[PMID: 28757062]
PC-3	IC₅₀	20.3 μM Compound: Flutamide	Anticancer activity against human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Anticancer activity against human PC-3 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 32866675]
PC-3	IC₅₀	58 μM Compound: Flutamide	Anticancer activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Anticancer activity against human PC-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 34425478]
SC-3	IC₅₀	4.2 μM Compound: 4, flutamide	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	7.2 x 10^-7 M Compound: 3	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	7.2 x 10^-1 μM Compound: 3	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]
Sf21	IC₅₀	143.2 μM Compound: Flutamide	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf21	IC₅₀	78.7 μM Compound: Flutamide	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
U-251	IC₅₀	22.11 μM Compound: Flutamide	Anticancer activity against human U-251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay Anticancer activity against human U-251 cells assessed as inhibition of cell growth incubated for 48 hrs by MTT assay	[PMID: 32866675]

In Vitro

The active metabolite of Flutamide, is Flutamide-OH. Both of them directly bind rat anterior pituitary androgen receptor (Ki=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].
Flutamide has cytotoxic activity against PC3 and LNCap (IC50s 20 μM and 12 μM, respectively). Flutamide (10 μM, 5 μM; 48 h) induces apoptosis and reduces cell migration and colonization in PC3 and LNCap cells^[4].
Flutamide also downregulates the expression of KLK2 and EMT pathway genes in cells^[4].

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

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^[5].
Flutamide (12.5-50 mg/kg; sc; once daily for 3 days) alleviates heat stroke in heat-stressed mice^[6].

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

Essai clinique

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

Chemical Information

CAS No. 13311-84-7
Appearance Solid
Masse moléculaire 276.21
Formule C₁₁H₁₁F₃N₂O₃
Color Light yellow to yellow
SMILES

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

SCH 13521
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

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Journal Impact Factor

J Hazard Mater

Medium-chain perfluoroalkyl carboxylic acids exert male reproductive toxicity at environmental and human exposure levels by antagonizing androgen receptor mediated pathways. [Abstract]

2025 Aug 10:496:139488. PMID: 40811912

Flutamide purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Aug 10:496:139488. [Abstract]

Flutamide (2000 μg/L; 28 d) caused widened interstitial spaces and vacuolation in zebrafish testis exposed to PFCAs.

Flutamide purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Aug 10:496:139488. [Abstract]

Flutamide (FT) (2000 μg/L; 28 d) significantly decreased serum T levels and increased E2 and VTG levels in zebrafish.

Flutamide purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Aug 10:496:139488. [Abstract]

Flutamide (FT) (2000 μg/L; 28 d) significantly downregulated androgen synthesis genes and AR pathway related genes (cyp17a1, star, hsd11b2, sox9a, ar and fkbp5) in zebrafish.

Flutamide purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Aug 10:496:139488. [Abstract]

Flutamide (FT) (1 nM-1 μM; 48 h) suppressed proliferation of LNCaP cells dose-dependently.

Flutamide purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2025 Aug 10:496:139488. [Abstract]

Flutamide (FT) (1 nM-1 μM; 24 h) effectively suppressed the transcriptional activity of hAR enhanced by DHT in MDA-kb₂ cells.
Research (Wash D C)

Regulating Integrin β1 to Restore Gonadotropin-Releasing Hormone-Tanycyte Unit Function in Polycystic Ovary Syndrome-Related Hypothalamic Dysregulation. [Abstract]

2025 Feb 19:8:0619. PMID: 39975575
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Environ Int

Disruption of zebrafish sex differentiation by emerging contaminants hexafluoropropylene oxides at environmental concentrations via antagonizing androgen receptor pathways. [Abstract]

2024 Jul 2:190:108868. PMID: 38976939
Acta Pharmacol Sin

Osimertinib successfully combats EGFR-negative glioblastoma cells by inhibiting the MAPK pathway. [Abstract]

2021 Jan;42(1):108-114. PMID: 32398685
Environ Health (Wash)

Distinctively Different Effects of Perfluorobutanoic Acid and Perfluorononanoic Acid on Zebrafish Sex Differentiation and Androgen Receptor Activity. [Abstract]

2025 Jan 27;3(5):482-492. PMID: 40400555
Ecotoxicol Environ Saf

Effect of bisphenol A on craniofacial cartilage development in zebrafish (Danio rerio) embryos: A morphological study. [Abstract]

2021 Apr 1:212:111991. PMID: 33548570
Biotechnol Bioeng

An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]

2021 Dec;118(12):4687-4698. PMID: 34478150
J Steroid Biochem Mol Biol

Dihydrotestosterone regulation of cyclooxygenase-2 expression in bovine endometrial epithelium cells by androgen receptor mediated EGFR/PI3K/Akt pathway. [Abstract]

2021 Nov:214:106001. PMID: 34547381
Biol Open

Drug repurposing to combat multidrug-resistant hookworm. [Abstract]

2026 Feb 15;15(2):bio062380. PMID: 41601273
SSRN

2025 Aug 9.
SSRN

2023 Apr 17.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (362.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

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

3.6204 mL

18.1022 mL

36.2043 mL

5 mM

0.7241 mL

3.6204 mL

7.2409 mL

10 mM

0.3620 mL

1.8102 mL

3.6204 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

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Calculateur de dilution

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 (9.05 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 (9.05 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 (9.05 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:

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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:

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
SDS (418 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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MS (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Simard J, et al. Characteristics of interaction of the antiandrogen flutamide with the androgen receptor in various target tissues. Mol Cell Endocrinol. 1986 Mar;44(3):261-70. [Content Brief]

[2]. Luthy IA, et al. Androgenic activity of synthetic progestins and spironolactone in androgen-sensitive mouse mammary carcinoma (Shionogi) cells in culture. J Steroid Biochem. 1988 Nov;31(5):845-52. [Content Brief]

[3]. Crawford ED, et al. A controlled trial of leuprolide with and without flutamide in prostatic carcinoma. N Engl J Med. 1989 Aug 17;321(7):419-24. [Content Brief]

[4]. Rahimnia R, et al. The effect of Ganoderma lucidum polysaccharide extract on sensitizing prostate cancer cells to flutamide and docetaxel: an in vitro study. Sci Rep. 2023 Nov 2;13(1):18940. [Content Brief]

[5]. Lin CY, et al. Flutamide, an androgen receptor antagonist, improves heatstroke outcomes in mice. Eur J Pharmacol. 2012 Aug 5;688(1-3):62-7. [Content Brief]

[6]. Marchetti B, et al. Characteristics of flutamide action on prostatic and testicular functions in the rat. J Steroid Biochem. 1988 Jun;29(6):691-8. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.6204 mL	18.1022 mL	36.2043 mL	90.5108 mL
	5 mM	0.7241 mL	3.6204 mL	7.2409 mL	18.1022 mL
	10 mM	0.3620 mL	1.8102 mL	3.6204 mL	9.0511 mL
	15 mM	0.2414 mL	1.2068 mL	2.4136 mL	6.0341 mL
	20 mM	0.1810 mL	0.9051 mL	1.8102 mL	4.5255 mL
	25 mM	0.1448 mL	0.7241 mL	1.4482 mL	3.6204 mL
	30 mM	0.1207 mL	0.6034 mL	1.2068 mL	3.0170 mL
	40 mM	0.0905 mL	0.4526 mL	0.9051 mL	2.2628 mL
	50 mM	0.0724 mL	0.3620 mL	0.7241 mL	1.8102 mL
	60 mM	0.0603 mL	0.3017 mL	0.6034 mL	1.5085 mL
	80 mM	0.0453 mL	0.2263 mL	0.4526 mL	1.1314 mL
	100 mM	0.0362 mL	0.1810 mL	0.3620 mL	0.9051 mL

Keywords

Flutamide

12 Cited Publications

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Flutamide

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Publications Citing Use of MedChemExpress (MCE) Flutamide

Activité biologique

Chemical Information

Publications (12)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Flutamide

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Transcription Factor-Targeted Library

Rare Diseases Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

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Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Flutamide

Activité biologique

Chemical Information

Publications (12)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Flutamide Related Classifications

Cat. No.: HY-B0022