Art. -Nr.: HY-16060

Apalutamide

(Synonyms: ARN-509)

15 Cited Publications

Kundenbewertung

Based on 15 publication(s) in Google Scholar

Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC₅₀ of 16 nM.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.94%
CAS. Nr.: 956104-40-8
Formel: C₂₁H₁₅F₄N₅O₂S
Molecular Weight:477.43

Speicherung:

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

Apalutamide Chemical Structure

CAS. Nr.: 956104-40-8

Größe

Preis

Verfügbarkeit

Menge

Sample (0.1mg)

In-stock

(In Japan)

Apply Now

Angebot einholen Ask For Quote & Lead Time Consult sales personnel for more information Check price and availability Angebot einholen Ask For Quote & Lead Time Consult sales personnel for more information Check price and availability

Massenanfrage

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (15)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC₅₀ of 16 nM^[1].

IC₅₀ & Target

IC50: 16 nM (Androgen receptor)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	CC₅₀	>50 μM Compound: ARN-509	Antiproliferative activity against African green monkey COS-7 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against African green monkey COS-7 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 38385428]
CWR22R	CC₅₀	>50 μM Compound: ARN-509	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 38385428]
DU-145	CC₅₀	>50 μM Compound: ARN-509	Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 38385428]
HEK293	IC₅₀	0.016 μM Compound: 6	Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay	[PMID: 30525603]
LNCaP	CC₅₀	9.72 μM Compound: ARN-509	Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 38385428]
LNCaP	IC₅₀	174 nM Compound: 5, ARN-509	Antiproliferative activity against human LNCAP cells after 3 days Antiproliferative activity against human LNCAP cells after 3 days	[PMID: 26046313]
LNCaP C4-2	CC₅₀	41.67 μM Compound: ARN-509	Antiproliferative activity against human C4-2 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against human C4-2 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 38385428]
PC-3	CC₅₀	>50 μM Compound: ARN-509	Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability measured after 72 hrs by CCK-8 method	[PMID: 38385428]

In Vitro

Apalutamide (ARN-509) also exhibits low micromolar affinity (IC₅₀ 3 μM) for the GABA_A receptor in radioligand binding-assays and thus may potentially antagonize GABA_A at therapeutic dose levels^[1]. Apalutamide is a potent androgen receptor (AR) antagonist that targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets^[2].

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

In Vivo

Apalutamide (ARN-509) exhibits low systemic clearance, high oral bioavailability and long plasma half-life in both mouse and dog, supporting once-daily oral dosing. Consistent with its long terminal-half-life, Apalutamide steady-state plasma-levels increases in repeat-dose studies, resulting in high C_24hr levels and low peak:trough ratios (ratio:2.5). Castrate male mice bearing LNCaP/AR xenograft tumors are treated with either Apalutamide at doses of 1, 10 or 30 mg/kg/day. Thirteen of 20 Apalutamide (30 mg/kg/day)-treated animals exhibit >50% reduction in tumor-volume at day 28 versus 3 of 19 MDV3100 (30 mg/kg/day)-treated mice^[1].

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. Nr. 956104-40-8
Appearance Solid
Molecular Weight 477.43
Formel C₂₁H₁₅F₄N₅O₂S
Color White to off-white
SMILES

O=C(NC)C1=CC=C(N(C(N(C2=CC(C(F)(F)F)=C(C#N)N=C2)C3=O)=S)C43CCC4)C=C1F
Synonyms

ARN-509
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (15)

All Cell Proliferation/Viability AssayIn Vivo Efficacy StudyHistological Imaging/Staining

Sort by:

Journal Impact Factor

Cell Death Dis

CRISPR screening identifies CDK12 as a conservative vulnerability of prostate cancer. [Abstract]

2021 Jul 27;12(8):740. PMID: 34315855

Apalutamide purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2021 Jul 27;12(8):740. [Abstract]

PCa cells were treated with the AR antagonist Apalutamide (Apa) (25 µM) in the colony formation assay.
NPJ Breast Cancer

Transcriptomic analysis to uncover the mechanism of radiosensitization of AR-positive triple-negative breast cancers with AR inhibition. [Abstract]

2026 Feb 24. PMID: 41735341

Apalutamide purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2026 Feb 24. [Abstract]

Apalutamide (ARN-509) (500 nM-2 μM; 1 h) radiosensitized AR+ TNBC MDA-MB-453 cells.

Apalutamide purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2026 Feb 24. [Abstract]

Clonogenic survival assay curves and radiation enhancement ratios (rER) with Apalutamide (ARN-509) (5 µM) of both sham transfected and ERK-overexpressing ACC-422 cells.
Br J Cancer

Androgen and oestrogen receptor co-expression determines the efficacy of hormone receptor-mediated radiosensitisation in breast cancer. [Abstract]

2022 Sep;127(5):927-936. PMID: 35618789
JCI Insight

Targeting castration-resistant prostate cancer with androgen receptor antisense oligonucleotide therapy. [Abstract]

2019 Sep 5;4(17):e122688. PMID: 31484823

Apalutamide purchased from MedChemExpress. Usage Cited in: JCI Insight. 2019 Sep 5;4(17):e122688. [Abstract]

Apalutamide (Apa) (30 mg/kg; once daily for 4 weeks). Plots of mean ± SEM of GUT and prostate weights of Pten-KO mice normalized to baseline means, and a waterfall plot of individual treatment response based on prostate tumor weight normalized to median baseline level.

Apalutamide purchased from MedChemExpress. Usage Cited in: JCI Insight. 2019 Sep 5;4(17):e122688. [Abstract]

Apalutamide (Apa) (30 mg/kg; once daily for 4 weeks). Representative images of whole genitourinary tracts and H&E-stained sections of dorsal prostate (DP) and ventral prostate (VP) tumors in Pten-KO mice.
Biosensors (Basel)

An Extracellular Matrix Overlay Model for Bioluminescence Microscopy to Measure Single-Cell Heterogeneous Responses to Antiandrogens in Prostate Cancer Cells. [Abstract]

2024 Apr 5;14(4):175. PMID: 38667168
Mol Cancer Ther

The Effect of F877L and T878A Mutations on Androgen Receptor Response to Enzalutamide. [Abstract]

2016 Jul;15(7):1702-12. PMID: 27196756
Chem Biol Interact

Inhibition of aldo-keto reductase 1C3 overcomes gemcitabine/cisplatin resistance in bladder cancer. [Abstract]

2024 Jan 25:388:110840. PMID: 38122923
Front Pharmacol

Icariin Ameliorates Diabetic Renal Tubulointerstitial Fibrosis by Restoring Autophagy via Regulation of the miR-192-5p/GLP-1R Pathway. [Abstract]

2021 Jul 19:12:720387. PMID: 34349660
Mol Cancer Res

Exploitation of Castration-Resistant Prostate Cancer Transcription Factor Dependencies by the Novel BET Inhibitor ABBV-075. [Abstract]

2017 Jan;15(1):35-44. PMID: 27707886
Drug Metab Dispos

Quantitative clinical risk assessment of CYP2C, UDP-glucuronosyltransferase, P-glycoprotein induction, and complex drug-drug interactions using TruVivo human hepatocyte triculture platform. [Abstract]

2025 Apr;53(4):100052. PMID: 40133023
Aging (Albany NY)

AAT resistance-related AC007405.2 and AL354989.1 as novel diagnostic and prognostic markers in prostate cancer. [Abstract]

2024 Apr 19;16(8):7249-7266. PMID: 38643469
Sci Rep

Drivers of AR indifferent anti-androgen resistance in prostate cancer cells. [Abstract]

2019 Sep 24;9(1):13786. PMID: 31551480
Arch Biochem Biophys

Artepillin C overcomes apalutamide resistance through blocking androgen signaling in prostate cancer cells. [Abstract]

2023 Feb:735:109519. PMID: 36642262
Prostate

MIF Facilitates Resistance to Androgen Deprivation Therapy by Regulating AMPD2 Expression in Prostate Cancer Cells. [Abstract]

2025 Sep 19. PMID: 40968720
Biomed Chromatogr

Assessment of Apalutamide Metabolic Stability in HLMs Matrix Using a Sensitive and Fast UPLC-MS/MS Method: In Silico Screening for Toxicity Alerts and Metabolic Lability. [Abstract]

2026 Mar;40(3):e70376. PMID: 41582395

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (104.73 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

2.0945 mL

10.4727 mL

20.9455 mL

5 mM

0.4189 mL

2.0945 mL

4.1891 mL

10 mM

0.2095 mL

1.0473 mL

2.0945 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.08 mg/mL (4.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.36 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Protokoll

Cell Assay^[1]

Trypsinized VCaP cells are adjusted to a concentration of 100,000 cells per mL in phenol-red-free RPMI 1640 (with 5% CSS), and dispensed in 16 µL aliquots into CellBIND 384 well plates. Cells are incubated for 48 hours, after which ligand is added in a 16 µL volume to the RPMI culture medium. For the antagonist mode assay, the ligands are diluted in culture medium also containing 30 pM R1881. After 7 days’ incubation, 16 µL of CellTiter-Glo Luminescent Cell Viability Assay is added and Relative Luminescence Units (RLUs) measured^[1].

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

Animal Administration^[1]

Mice^[1]
In vivo xenograft experiments to determine anti-tumor response are carried out in SHO SCID male mice. Mice are orchiectomized under isoflorane anesthesia and are given 2-3 days to recover prior to tumor cell injection. LNCaP/AR(cs) cells are suspended in 50% RPMI, 50% Matrigel, and 5×10⁶ cells/xenograft are injected in a volume of 100 μL. Animals are observed weekly until tumor growth is apparent. From 24 d post-injection, tumors are measured weekly, and after 40-60 days post-injection, animals are randomized into cohorts of equivalent mean (150-250 mm³) and range tumor burden. All compounds (e.g., Apalutamide, 30 mg/kg per day) are administered daily by oral gavage. Statistical analyses are performed using Graphpad Prism.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 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)
- 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)

Verweise

[1]. Clegg NJ, et al. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012 Mar 15;72(6):1494-503. [Content Brief]

[2]. Smith MR, et al. Phase 2 Study of the Safety and Antitumor Activity of Apalutamide (ARN-509), a Potent Androgen Receptor Antagonist, in the High-risk Nonmetastatic Castration-resistant Prostate Cancer Cohort. Eur Urol. 2016 May 6. pii: S0302-2838(16)30133 [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	2.0945 mL	10.4727 mL	20.9455 mL	52.3637 mL
	5 mM	0.4189 mL	2.0945 mL	4.1891 mL	10.4727 mL
	10 mM	0.2095 mL	1.0473 mL	2.0945 mL	5.2364 mL
	15 mM	0.1396 mL	0.6982 mL	1.3964 mL	3.4909 mL
	20 mM	0.1047 mL	0.5236 mL	1.0473 mL	2.6182 mL
	25 mM	0.0838 mL	0.4189 mL	0.8378 mL	2.0945 mL
	30 mM	0.0698 mL	0.3491 mL	0.6982 mL	1.7455 mL
	40 mM	0.0524 mL	0.2618 mL	0.5236 mL	1.3091 mL
	50 mM	0.0419 mL	0.2095 mL	0.4189 mL	1.0473 mL
	60 mM	0.0349 mL	0.1745 mL	0.3491 mL	0.8727 mL
	80 mM	0.0262 mL	0.1309 mL	0.2618 mL	0.6545 mL
	100 mM	0.0209 mL	0.1047 mL	0.2095 mL	0.5236 mL

Keywords

Apalutamide

15 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Apalutamide

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Targeted Therapy Drug Library

Transcription Factor-Targeted Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Cysteine Targeted Covalent Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

Cardiotoxic Compound Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Apalutamide

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Apalutamide

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Targeted Therapy Drug Library

Transcription Factor-Targeted Library

EMA-Approved Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Cysteine Targeted Covalent Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

Cardiotoxic Compound Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Apalutamide

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Apalutamide Related Classifications

Art. -Nr.: HY-16060