Catalog No.S2840

ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.

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ARN-509 Chemical Structure

ARN-509 Chemical Structure
Molecular Weight: 477.43

Validation & Quality Control

Quality Control & MSDS

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Product Information

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Product Description

Biological Activity

Description ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.
Targets Androgen Receptor [1]
(Cell-free assay)
GABAA receptor [1]
(Cell-free assay)
IC50 16 nM 3 μM
In vitro ARN-509 (< 10 μM) inhibits androgen-mediated induction or repression of mRNA expression levels for 13 endogenous genes including PSA and TMPRSS2 in the LNCaP/AR prostate cancer cell line. ARN-509 (< 10 μM) inhibits the proliferative effect of R1881 (30 pM) in the LNCaP/AR prostate cancer cell line. ARN-509 (10 μM) impairs AR nuclear localization and thus reduces the concentration of AR available to bind androgen response elements (ARE) in LNCaP cells expressing AR-EYFP. ARN-509 (10 μM) is able to effectively compete with R1881 (1 nM) and prevent AR from binding to promoter regions. ARN-509 inhibits R1881-induced VP16-AR–mediated transcription with IC50 of 0.2 μM in Hep-G2 cells expressing a VP16-AR fusion protein and an ARE-driven luciferase reporter. [1]
In vivo ARN-509 (10 mg/kg/d, oral) inhibits tumor growth with decreased proliferative index and increased apoptotic rate in castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors. ARN-509 dose dependently inhibits tumor growth with highest efficacy at dose of 30 mg/kg/day in castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors. ARN-509 dosed at 10 mg/kg/d for 28 days results in a 3-fold reduction in prostates weight associated with lacking glandular secretory activity and 1.7-fold reduction in epididymis weight in adult male dogs. ARN-509 (10 mg/kg/d, oral) inhibits cell proliferation of prostate tissues in adult male dogs. [1] ARN-509 is safe and well tolerated in 24 patients with metastatic CRPC who has progressed on prior treatments and peak plasma concentrations occurred 2 to 3 hours after administration. ARN-509 results in durable PSA declines at doses ranging from 30 to 300 mg in patients with metastatic CRPC. [2] ARN-509 shows powerful anti-cancer activity and induces durable remissions long after therapy completion in castrate resistant prostate cancer mouse models. [3]

Protocol(Only for Reference)

Cell Assay: [1]

Cell lines LNCaP/AR prostate cancer cell line
Concentrations 10 μM
Incubation Time 48 hours
Method Cells are incubated for 48 hours, after which ARN-509 is added in a 16 μL volume to the RPMI culture medium. For the antagonist mode assay, the ARN-509 is 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.

Animal Study: [1]

Animal Models Castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors
Formulation 15% Vitamin E-TPGS and 65% of a 0.5% w/v CMC solution in 20 mM citrate buffer (pH 4.0)
Dosages 30 mg/kg/day
Administration Orally

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Clegg NJ, et al. Cancer Res, 2012, 72(6), 1494-1503.

[2] Dana E, et al, 2012, Genitourinary Cancers Symposium. Abst 43.

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Clinical Trial Information( data from, updated on 2016-05-07)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02703623 Not yet recruiting Prostate Cancer M.D. Anderson Cancer Center|Bristol-Myers Squibb|Janssen,  ...more M.D. Anderson Cancer Center|Bristol-Myers Squibb|Janssen, LP|Sanofi June 2016 Phase 2
NCT02721979 Not yet recruiting Stage II Prostate Adenocarcinoma University of Washington|National Cancer Institute (NCI) April 2016 Phase 2
NCT02106507 Recruiting Prostate Cancer Memorial Sloan Kettering Cancer Center|Aragon Pharmaceuti  ...more Memorial Sloan Kettering Cancer Center|Aragon Pharmaceuticals, Inc. April 2014 Phase 1
NCT01946204 Recruiting Prostatic Neoplasms Aragon Pharmaceuticals, Inc. October 2013 Phase 3
NCT01822041 Completed Healthy Aragon Pharmaceuticals, Inc. March 2013 Phase 1

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Chemical Information

Download ARN-509 SDF
Molecular Weight (MW) 477.43


CAS No. 956104-40-8
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 18 mg/mL (37.7 mM)
Ethanol 5 mg/mL (10.47 mM)
Water <1 mg/mL (<1 mM)
In vivo 0.5% CMC, pH4.0 14 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Benzamide, 4-[7-[6-cyano-5-(trifluoromethyl)-3-pyridinyl]-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methyl-

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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