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    Darolutamide (ODM-201;BAY-1841788)
    Darolutamide (ODM-201;BAY-1841788)

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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 #: V1765
    CAS #: 1297538-32-9Purity ≥98%

    Description: Darolutamide (formerly known as BAY-1841788; ODM-201; BAY1841788; Nubeqa) is a novel and potent androgen receptor (AR) antagonist with potential antitumor activity. It inhibits AR nuclear translocation with a Ki of 11 nM in competitive AR binding assays. In AR-HEK293 cells stably expressing full-length human AR (hAR) and an androgen-responsive luciferase reporter gene construct. In human U2-OS osteosarcoma cells expressing wtAR or mutant AR(F876L), AR(W741L), or AR(T877A), ODM-201 and ORM-15341 also functioned as full antagonists. 

    References: Sci Rep. 2015 Jul 3;5:12007.

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    • 香港大学
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    Molecular Weight (MW)398.85
    FormulaC19H19ClN6O2
    CAS No.1297538-32-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 80 mg/mL (200.6 mM)
    Water: <1 mg/mL
    Ethanol: 38 mg/mL d (95.3 mM) 
    SMILESO=C(C1=NNC(C(O)C)=C1)N[[email protected]@H](C)CN2N=C(C3=CC=C(C#N)C(Cl)=C3)C=C2
    SynonymsBAY-1841788; ODM-201; BAY 1841788; ODM 201; BAY1841788; Nubeqa; ODM201


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    In Vitro

    In vitro activity: In AR-HEK293 cells stably expressing full-length hAR, ODM-201 inhibits human AR (hAR) with IC50 of 26 nM. ODM-201 inhibits VCaP cell proliferation with IC50 of 230 nM, while has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells.


    Kinase Assay: AR binding affinities of test compounds are studied in cytosolic lysates obtained from ventral prostates of castrated rats by a competition binding assay. Fresh prostates are minced and homogenized with Buffer A containing protease inhibitors. The homogenates are centrifuged and the resultant supernatants are treated with a dextran-coated charcoal solution to remove endogenous steroids. The dissociation constant of the radio ligand [3H]mibolerone for isolated rat ARs is determined in a saturation binding experiment. For the determination of Ki values, prostate cytosol preparations and 1 nM [3H]mibolerone are incubated with increasing concentrations of test compounds overnight. After the incubation, bound and free steroids are separated by treatment with 100 μL of dextran-coated charcoal suspension. Bound radioactivity is determined by counting 100 μL of supernatant fraction in 200 μL of scintillation fluid using a microbeta counter. All procedures are carried out at 0–4 °C.


    Cell Assay: VCaP cells are treated with a submaximal concentration of mibolerone (0.1 nM) and increasing concentrations of test compounds in steroid-free assay medium supplemented with 4 mM GlutaMAX. After a 4-day incubation with the compounds, cell viability is measured using a WST-1 cell proliferation assay. To rule out non-AR –mediated toxicity, AR-negative PC cells (DU-145) and lung cancer cells (H1581) are treated with an increasing concentration of ODM-201, and cell viability is measured as described above.

    In VivoIn mice bearing VCaP xenografts, ODM-201 (50 mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth.
    Animal modelBALB/c nude male mice bearing VCaP xenografts
    Formulation & DosageDissolved in Macrocol + propylene glycol +5% glucose (50:30:20, v/v/v); 50 mg/kg; p.o. administration
    References

    Sci Rep. 2015 Jul 3;5:12007.


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

    ODM-201

    The activation (A) or inhibition (B) of mutant AR(F876L), AR(W741L), and AR(T877A). Sci Rep. 2015 Jul 3;5:12007.
     

    ODM-201

    The inhibition of the nuclear translocation of AR. Sci Rep. 2015 Jul 3;5:12007.
     

    ODM-201

    Growth inhibition of VCaP cells in in vitro and in vivo CRPC settings. Sci Rep. 2015 Jul 3;5:12007.


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