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    AZD3514
    AZD3514

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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 #: V1766
    CAS #: 1240299-33-5Purity ≥98%

    Description: AZD3514 (AZD-3514; AZD 3514) is a novel, potent and orally bioavailable androgen receptor downregulator with potential anticancer activity. It inhibits AR with Ki of 2.2 μM and has the ability to reduce AR protein expression and thus has the potential to be used as an anticancer agent. In LNCaP and LAPC4 prostate cancer cells, AZD3514 inhibited DHT-driven proliferation of LNCaP cells in a dose-dependent way and inhibited the ligand-driven expression of AR-regulated genes PSA and TMPRSS2. Also, AZD3514 reduced AR protein expression in a dose-dependent way. AZD3514 is being studied in a Phase I clinical trial to treat patients with castrate-resistant prostate cancer.

    References: Bioorg Med Chem Lett. 2013 Apr 1;23(7):1945-8; Mol Cancer Ther. 2013 Sep;12(9):1715-27.

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    Molecular Weight (MW)519.56
    FormulaC25H32F3N7O2 
    CAS No.1240299-33-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (192.5 mM)
    Water: <1 mg/mL
    Ethanol: 100 mg/mL (192.5 mM)
    Other InfoChemical Name: 1-(4-(2-(4-(1-(3-(trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenoxy)ethyl)piperazin-1-yl)ethanone
    InChi Key: JMEYDSHPKCSIJC-UHFFFAOYSA-N
    InChi Code: InChI=1S/C25H32F3N7O2/c1-18(36)33-14-12-32(13-15-33)16-17-37-21-4-2-19(3-5-21)20-8-10-34(11-9-20)23-7-6-22-29-30-24(25(26,27)28)35(22)31-23/h2-5,20H,6-17H2,1H3
    SMILES Code: CC(N1CCN(CCOC2=CC=C(C3CCN(C4=NN5C(CC4)=NN=C5C(F)(F)F)CC3)C=C2)CC1)=O
    SynonymsAZD3514; AZD 3514; AZD-3514.


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    In Vitro

    In vitro activity: AZD3514 binds to the AR ligand binding domain and has selectivity for binding to AR over other nuclear hormone receptors. In vitro AZD3514 inhibits cell growth in prostate cancer cells expressing wild-type (VCaP) and mutated (T877A) AR (LNCaP), but is inactive in AR-negative prostate cancer cells. AZD3514 causes a rapid reduction in PSA synthesis in vitro; with a significant decrease in PSA mRNA being evident in LNCaP cells within 2-3 h of compound treatment. AZD3514 inhibits an androgen-induced translocation of AR from the cytoplasm to the nucleus within a comparable time-frame in LNCaP cells and U2OS AR-transfected cells. AZD3514 treatment also reduces AR protein in LNCaP cells maintained in steroid-depleted conditions; an effect which is evident within 6-8 h, and maximal at 18-24 h. The ability to down-regulate AR under such conditions differentiates AZD3514 from the AR antagonists bicalutamide and Enzalutamide, which do not reduce AR protein levels.


    Kinase Assay: AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression. 


    Cell Assay: In LNCaP and LAPC4 prostate cancer cells, AZD3514 inhibited DHT-driven proliferation of LNCaP cells in a dose-dependent way and inhibited the ligand-driven expression of AR-regulated genes PSA and TMPRSS2. Also, AZD3514 reduced AR protein expression in a dose-dependent way.  

    In VivoOral administration of AZD3514 (100mg/kg once-daily for 7 days) significantly inhibits testosterone-induced growth of sexual accessory organs. The mode of action of AZD3514 is associated with loss of AR function. Administration of AZD3514 (100 mg/kg/day orally) for 3 days to Copenhagen rats bearing R3327H Dunning prostate tumours, indicates that AZD3514 treatment also reduces tumour AR in vivo.
    Animal model Rats
    Formulation & Dosage 100mg/kg; Oral
    ReferencesBioorg Med Chem Lett. 2013 Apr 1;23(7):1945-8; Mol Cancer Ther. 2013 Sep;12(9):1715-27.


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

    AZD3514

    (A-B) LNCaP cells treated with AZD3514 for 24 hours. Graph shows AR levels normalized to GAPDH and relative to the vehicle control.  2013 Sep;12(9):1715-27.

    AZD3514

    (A-B) LNCaP cells grown in steroid free conditions in SILAC media containing 5% dialyzed fetal calf serum, 13C615N4 arginine and 13C6 lysine (to label proteins as “heavy”) were treated with 10 μM AZD3514 or vehicle for 24 hours, then switched to grow in SILAC media containing unlabeled arginine (to label newly synthesized protein as “light”).  2013 Sep;12(9):1715-27.
     


    AZD3514

    (A-D) AZD3514 was administered by oral gavage once daily to Copenhagen rats bearing established R3327H tumors at the doses indicated. (A) tumor volumes are plotted against time.  2013 Sep;12(9):1715-27.


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