ARN-509

Catalog No.S2840 1 Product Citations

ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, 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, useful for prostate cancer treatment. Phase 3.
Targets Androgen Receptor GABAA receptor
IC50 16 nM [1] 3 μM [1]
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]
Features

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
Solubility 0.5% CMC, pH4.0, , 14 mg/mL
* 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.
1

References

[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 http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01822041 Completed Healthy Aragon Pharmaceuticals, Inc. 2013-03 Phase 1
NCT01946204 Recruiting Prostatic Neoplasms Aragon Pharmaceuticals, Inc. 2013-09 Phase 3
NCT02031666 Recruiting Healthy Janssen Research & Development, LLC 2013-12 Phase 1
NCT02106507 Recruiting Prostate Cancer Memorial Sloan-Kettering Cancer Center|Aragon Pharmaceuticals, Inc. 2014-04 Phase 1
NCT02123758 Not yet recruiting Prostatic Neoplasms|Metastatic Castration-Resistant Prostate Cancer (mCRPC) Aragon Pharmaceuticals, Inc. 2014-06 Phase 1

Chemical Information

Download ARN-509 SDF
Molecular Weight (MW) 477.43
Formula

C21H15F4N5O2S

CAS No. 956104-40-8
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms
Solubility (25°C) * In vitro DMSO 18 mg/mL (37 mM)
Water <1 mg/mL (<1 mM)
Ethanol 5 mg/mL (10 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-

Research Area

Product Citations (1)

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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