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    Apalutamide (ARN-509)
    Apalutamide (ARN-509)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1760
    CAS #: 956104-40-8Purity ≥98%

    Description: Apalutamide (formerly JNJ56021927; ARN509; JNJ-56021927; ARN-509; trade name Erleada), an approved anticancer drug, is a potent, selective and competitive, orally bioavailable AR/androgen receptor inhibitor with an IC50 of 16 nM in a cell-free assay. In February 2018, Apalutamide received approval from FDA for the treatment of prostate cancer (non-metastatic castration-resistant PC-nmCRPC). Apalutamide is specifically indicated for use in conjunction with castration in the treatment of nmCRPC. The mechanism of action is to bind directly to the ligand-binding domain of the AR and block the effects of androgens. 

    References:  2018 Apr;78(6):699-705; Cancer Res. 2012 Mar 15;72(6):1494-503.

    Related CAS #: 956104-40-8 (free base)   1505451-77-3 (DMSO)   2376466-25-8 (acetate)   1505451-73-9 (ethanol)  1505451-74-0 (hydrate)   1505451-73-9 (ethanol)

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    Molecular Weight (MW)477.43
    FormulaC21H15F4N5O2S
    CAS No.956104-40-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: >20 mg/mL
    Water: <1 mg/mL
    Ethanol: 5 mg/mL (10.5 mM)
    Solubility (In vivo)0.5% CMC, pH4.0: 14 mg/mL 
    Synonyms

    JNJ56021927; ARN509; JNJ-56021927; ARN 509; JNJ 56021927; ARN-509; Apalutamide; Brand name: Erleada

    Chemical Name: 4-(7-(6-cyano-5-(trifluoromethyl)pyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]octan-5-yl)-2-fluoro-N-methylbenzamide 

    SMILES Code: 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 

    Exact Mass: 477.08826 


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    In Vitro

    In vitro activity: Apalutamide (brand name Erleada), previously known as ARN-509 and JNJ-56021927, is a potent, selective and competitive, orally bioavailable androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay. 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.


    Kinase Assay: Competitor assay kits (green) are used to determine relative in vitro binding affinities of ARN-509 for the rat AR ligand binding domain (LBD), human progesterone receptor (PR) LBD, and full-length human estrogen receptor-alpha (ERα) and human glucocorticoid receptor (GR). Each hormone dose is performed in triplicate, relative error is calculated from the standard error of the mean (SEM), and binding curves are fit using a single binding site competition model (Prism statistical analysis software package) with R2>0.8. Experiments are conducted multiple times with SEM<0.3 log units from the average logIC50 value. Ki values are calculated as averages across experiments with SEM, and binding affinities are reported as a percentage relative to the tight-binding ligand control for that receptor.


    Cell Assay: 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.

    In VivoARN-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. 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. ARN-509 shows powerful anti-cancer activity and induces durable remissions long after therapy completion in castrate resistant prostate cancer mouse models. 
    Animal modelCastrate male immunodeficient mice harboring LNCaP/AR-luc xenograft tumors
    Formulation & DosageDissolved in 15% Vitamin E-TPGS and 65% of a 0.5% w/v CMC solution in 20 mM citrate buffer (pH 4.0), and diluted in saline; 30 mg/kg/day; oral administration
    ReferencesCancer Res. 2012 Mar 15;72(6):1494-503; J Biol Chem. 1999 Jun 4;274(23):16147-52.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    ARN-509


    ARN-509 activity in vitro in human prostate-cancer cells.  2012 Mar 15;72(6):1494-503. 

     ARN-509


    ARN-509 impairs AR nuclear-localization and inhibits DNA-binding.  2012 Mar 15;72(6):1494-503.

     ARN-509


    ARN-509 is active in models of castration-resistant prostate cancer.  2012 Mar 15;72(6):1494-503.

    ARN-509


    ARN-509 achieves similar efficacy with lower steady-state plasma-levels than MDV3100 in LNCaP/AR xenograft models of castration-resistant prostate cancer.  2012 Mar 15;72(6):1494-503.

     

     ARN-509


    ARN-509 induces castrate-like changes in dog prostate and epididymis.  2012 Mar 15;72(6):1494-503.



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