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ARN-509 Androgen receptor inhibitor

Catalog No.A8364
Size Price Stock Qty
10mM (in 1mL DMSO)
$105.00
In stock
5mg
$80.00
In stock
10mg
$140.00
In stock
50mg
$350.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Bao D, Cheng C, et al. "Regulation of p53wt glioma cell proliferation by androgen receptor-mediated inhibition of small VCP/p97-interacting protein expression."Oncotarget. 2017 Apr 4;8(14):23142-23154. PMID:28423563
2. Sun J, Wang D, et al. "Androgen Receptor Regulates the Growth of Neuroblastoma Cells in vitro and in vivo." Front Neurosci. 2017 Mar 7;11:116. PMID:28326012

Quality Control

Quality Control & MSDS

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Chemical structure

ARN-509

Related Biological Data

ARN-509

Related Biological Data

ARN-509

Biological Activity

Description ARN-509 is a selective and competitive inhibitor of androgen receptor with an IC50 value of 16 nM.
Targets Androgen Receptor GABAA receptor        
IC50 16 nM 3 μM        

Protocol

Cell experiment [1]:

Cell lines

LNCaP, LNCaP-AR and VCaP cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

1 μM; 48 hrs

Applications

In LNCaP, LNCaP-AR and VCaP cells, ARN-509 increased DNA damage. In LNCaP cell line, ARN-509 decreased cell survival. In addition, ARN-509 significantly decreased C-NHEJ-mediated recombination (> 60%) in LNCaP cells that had been transfected with V(D)J recombination substrate along with RAG1 and RAG2 expression vectors.

Animal experiment [2]:

Animal models

Castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors

Dosage form

10 mg/kg/d; p.o.; for 17 days

Applications

In castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors, the 17-day Oral treatment with ARN-509 (10 mg/kg/d) consistently reduced androgen-driven luciferase reporter-gene activity. In addition, ARN-509 decreased the proliferative index and increased the apoptotic rate of tumors, respectively.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. William R. Polkinghorn, Joel S. Parker, Man X. Lee, et al. Androgen Receptor Signaling Regulates DNA Repair in Prostate Cancers. Cancer Discovery, 2013, 3(11):1245-53.

[2]. Nicola J. Clegg, John Wongvipat, James D. Joseph, et al. ARN-509: A Novel Antiandrogen for Prostate Cancer Treatment. Therapeutics, Targets & Chemical Biology, 2012, 72(6): 1494-1503.

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Chemical Properties

Cas No. 956104-40-8 SDF Download SDF
Synonyms ARN 509; ARN509
Chemical Name 4-[7-[6-cyano-5-(trifluoromethyl)pyridin-3-yl]-8-oxo-6-sulfanylidene-5,7-diazaspiro[3.4]octan-5-yl]-2-fluoro-N-methylbenzamide
Canonical SMILES CNC(=O)C1=C(C=C(C=C1)N2C(=S)N(C(=O)C23CCC3)C4=CN=C(C(=C4)C(F)(F)F)C#N)F
Formula C21H15F4N5O2S M.Wt 477.43
Solubility >23.9mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

ARN-509, a synthetic biaryl thiohydantoin compound, is a competitive androgen receptor (AR) inhibitor and fully antagonistic to AR overexpression. The IC50 of ARN-509 is 16 nmol/L [1].
AR, included in the steroid receptor superfamily, is important for prostate cell proliferation and male sexual differentiation [2]. AR overexpression is a common and important feature of castration resistant prostate cancer (CRPC) [1].
ARN-509 (1 μmol/L) treatment for 48 hours resulted in increased DNA damage in LNCaP cells, LNCaP-AR cells and VCaP cells. In LNCaP cell line, treatment with ARN-509 (1 μmol/L) resulted in decreased cell survival. Treatment with ARN-509 (1 μmol/L) for 48 hours significantly decreased C-NHEJ–mediated recombination (>60%) in LNCaP cells that had been transfected with V(D)J recombination substrate along with RAG1 and RAG2 expression vectors [3]. ARN-509 showed robust transcriptional and proliferative agonist activity in AR F876L–expressing cells, and promoted AR DNA binding in LNCaP/SRαF876L cells [4].
Orally treated with ARN-509 (10 mg/kg/d) for 17 days, androgendriven luciferase reporter–gene activity in castrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors (coexpressing exogenous AR and the AR-dependent reporter ARR2-Pb-luc), was consistently reduced. This indicated that ARN-509 inhibited AR in vivo. ARN-509 made tumors exhibit a decrease in proliferative index and an increase in apoptotic rate [1].
References:
[1]. Nicola J. Clegg, John Wongvipat, James D. Joseph, et al. ARN-509: A Novel Antiandrogen for Prostate Cancer Treatment. Therapeutics, Targets & Chemical Biology, 2012, 72(6): 1494-1503.
[2]. Shuyuan Yeh and Chawnshang Chang. Cloning and characterization of a specific coactivator, ARA70, for the androgen receptor in human prostate cells. Proc. Natl. Acad. Sci., 1996, 93: 5517-5521.
[3]. William R. Polkinghorn, Joel S. Parker, Man X. Lee, et al. Androgen Receptor Signaling Regulates DNA Repair in Prostate Cancers. Cancer Discovery, 2013, 3(11):1245-53.
[4]. James D. Joseph, Nhin Lu, Jing Qian, et al. A Clinically Relevant Androgen Receptor Mutation Confers Resistance to Second-Generation Antiandrogens Enzalutamide and ARN-509. Cancer Discovery, 2013, 3(9):1020-9.