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    NMS-E973
    NMS-E973

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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 #: V0884
    CAS #: 1253584-84-7Purity ≥98%

    Description: NMS-E973 (NMSE973; NMSE 973) is a novel, potent and selective HSP90 (Heat Shock Protein 90) inhibitor with potential antitumor activity. It inhibits HSP90 with a DC50 of<10 nM, and shows no activiy against a panel of protein kinases. NMS-E973 shows potent anti-proliferative activity in vitro against various cancer cell lines such as A2780 tumor cell line and BT-474 breast cancer cells with IC50 values of 69nM and 110nM, respectively. It exhibits excellent in vivo antitumor efficacy in mice bearing A2780 xenografts, with a TGI of 53% at 30mg/kg.

    References: Clin Cancer Res. 2013 Jul 1;19(13):3520-32; Bioorg Med Chem. 2013 Nov 15;21(22):7047-63. 

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    Molecular Weight (MW)454.43
    FormulaC22H22N4O7
    CAS No.1253584-84-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 90 mg/mL (198.1 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILESO=C(C1=NOC(C2=C(OC3=CC=C([N+]([O-])=O)C=C3)C=C(O)C=C2O)=C1)NC4CCN(C)CC4
    SynonymsNMSE973; NMS E973; NMS-E973; 


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    In Vitro

    In vitro activity: NMS-E973 shows a widespread antiproliferative activity with an average IC50 of 1.6 μM, and induces the degradation of client protein, such as Flt3, B-Raf, AKT, which further blocks tumor-related pathways, such as the Raf/MAPK, PI3K/AKT, and JAK/STAT pathways.


    Kinase Assay: For competition experiments, a protein concentration of 5 nM for Hsp90 and of 200 nM for Trap1 are mixed with 0.5 nmol/L probe (final concentrations). After incubation, the dimethyl sulfoxide (DMSO) compound solution is added to the mixture. The plate is incubated for 18 hours at room temperature and then the fluorescence polarization signal was measured. Data are fitted with the program Dynafit version 3.28.039 or SigmaPlot (SSI) using the mathematical equation for competitive binding of 2 ligands to the receptor.


    Cell Assay: NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of<10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases. NMS-E973 exerts antiproliferation effects on A2780 tumor cell line and BT-474 breast cancer cell line with IC50 values of 69nM and 110nM, respectively. When treated with mice bearing A2780 xenografts, the intravenous administration of NMS-E973 significantly inhibits tumor growth with TGI value of 53% at dose of 30mg/kg.

    In VivoNMS-E973 (10 mg/kg i.v.) shows a favorable pharmacokinetic profile with selective retention in tumor tissue and ability to cross the BBB. NMS-E973 (60 mg/kg i.v.) shows high antitumor efficacy in all the models tested, including A375 and A2780 xenografts. In addition, NMS-E973 (10 mg/kg i.v.) together with B-Raf inhibitor PLX-4720 at 100 mg/kg produces a synergic anti-tumor effect. In a mouse model of human ovarian cancer, NMS-E973 produces the antitumor activity by inhibition of Hsp90.
    Animal modelMice bearing A375 xenografts, A2780 xenografts, MOLM-13 xenografts or RKO xenografts.
    Formulation & DosageDissolved in 10% Tween 80 in 5% dextrose solution; 60 mg/kg; i.v.
    ReferencesClin Cancer Res. 2013 Jul 1;19(13):3520-32; Bioorg Med Chem. 2013 Nov 15;21(22):7047-63.


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

    NMS-E973

    Antitumor efficacy of NMS-E973 in A2780 model (7 mice/group). Clin Cancer Res.2013 Jul 1;19(13):3520-32.
      

    NMS-E973

    A, A375-LUC intracranial model: MRI scans of 6 representative mice, 3 controls and 3 mice treated with NMS-E973. Clin Cancer Res.2013 Jul 1;19(13):3520-32.
     

    NMS-E973

    A, antitumor efficacy of NMS-E973 administered 60 mg/Kg twice daily, 3-1-3, on-off-on, to 7 SCID mice inoculated subcutaneously with the MOLM-13 cells.


    NMS-E973

    A, combination experiment of NMS-E973 with PLX-4720. Clin Cancer Res. 2013 Jul 1;19(13):3520-32.


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