Apalutamide (Synonyms: ARN-509)

Name: Apalutamide
Brand: MedChemExpress
SKU: HY-16060
Rating: 5.0 (15 reviews)

Cat. No.: HY-16060 Purity: 99.94%: Data Sheet
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Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC₅₀ of 16 nM.

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

CAS No. : 956104-40-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 15 publication(s) in Google Scholar

Other Forms of Apalutamide:

15 Publications Citing Use of MCE Apalutamide

Cell Proliferation/Viability Assay

In Vivo Efficacy Study

Histological Imaging/Staining

: Apalutamide purchased from MedChemExpress. Usage Cited in: NPJ Breast Cancer. 2026 Feb 24.; 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.; 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.

: 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.

: 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.

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Biological Activity
Protocol
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References
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Description

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

Molecular Weight

477.43

Formula

C₂₁H₁₅F₄N₅O₂S

CAS No.

956104-40-8

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

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: ≥ 2.08 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.
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% 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

mg/kg

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(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: 99.94%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (252 KB) HNMR (117 KB) RP-HPLC (226 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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]

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]. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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]

Complete Stock Solution Preparation Table

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

Apalutamide 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:

Apalutamide956104-40-8ARN-509ARN509ARN 509Androgen ReceptorInhibitorinhibitorinhibit

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Apalutamide (Synonyms: ARN-509)

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Other Forms of Apalutamide:

Apalutamide Related Antibodies

15 Publications Citing Use of MCE Apalutamide

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Apalutamide Related Antibodies

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Complete Stock Solution Preparation Table

Apalutamide Related Classifications

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