ARN-509

Catalog No.S2840

ARN-509 Chemical Structure

Molecular Weight(MW): 477.43

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.

Size Price Stock Quantity  
In DMSO USD 400 In stock
USD 210 In stock
USD 270 In stock
USD 970 In stock

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1 Customer Review

  • J Cancer, 2014, 5(2):133-42.. ARN-509 purchased from Selleck.

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Choose Selective Androgen Receptor Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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)
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

Cell Research:[1]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 18 mg/mL (37.7 mM)
Ethanol 5 mg/mL (10.47 mM)
Water <1 mg/mL
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 Information

Molecular Weight 477.43
Formula

C21H15F4N5O2S

CAS No. 956104-40-8
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02949284 Not yet recruiting Stage II Prostate Adenocarcinoma|Stage III Prostate Adenocarcinoma Rutgers, The State University of New Jersey|National Cancer Institute (NCI) June 2017 Phase 2
NCT02721979 Not yet recruiting Stage II Prostate Adenocarcinoma University of Washington|National Cancer Institute (NCI) December 2016 Phase 2
NCT02770391 Recruiting Prostate Cancer Case Comprehensive Cancer Center October 2016 Phase 2
NCT02849990 Not yet recruiting Stage III Prostate Adenocarcinoma|Stage III Prostate Cancer|Stage IV Prostate Adenocarcinoma|Stage IV Prostate Cancer University of Washington|National Cancer Institute (NCI)|Janssen Scientific Affairs, LLC October 2016 Phase 2
NCT02772588 Recruiting Prostate Cancer Memorial Sloan Kettering Cancer Center|Janssen Pharmaceuticals|Weill Medical College of Cornell University|University of Michigan May 2016 Phase 2
NCT02703623 Recruiting Prostate Cancer M.D. Anderson Cancer Center|Bristol-Myers Squibb|Janssen, LP|Sanofi May 2016 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID