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    VER-49009
    VER-49009

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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 #: V0886
    CAS #: 558640-51-0Purity ≥98%

    Description: VER-49009 (CCT0129397; VER 49009; CCT-0129397; VER49009), a pyrazole-based compound, is a novel, potent and selective inhibitor of HSP90 (Heat Shock Protein 90) with potential antitumor activity. It inhibits HSP90β with an IC50 of 47 nM. It shows high in vivo antitumor efficacy in ice bearing established OVCAR3 human ovarian xenografts.

    References: Mol Cancer Ther. 2007 Apr;6(4):1198-211; Mol Cell Biochem. 2009 Oct;330(1-2):181-5. 

    Related CAS: 940289-57-6

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    Molecular Weight (MW)387.82
    FormulaC19H18ClN3O4
    CAS No.558640-51-0;
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 77 mg/mL (198.5 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    SMILES CodeO=C(C1=C(C2=CC=C(OC)C=C2)C(C3=CC(Cl)=C(O)C=C3O)=NN1)NCC
    SynonymsCCT0129397; CCT-0129397; CCT 0129397; VER 49009; VER49009; VER-49009.


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    In Vitro

    In vitro activity: VER-49009 inhibits the intrinsic ATPase activity of recombinant yeast Hsp90 with IC50 of 167 nM, and produces antiproliferative activity in a panel of human cancer cell lines and nontumorigenic cells in vitro. VER-49009 causes induction of HSP72 and HSP27 with depletion of client proteins, including C-RAF, B-RAF, and survivin, and PRMT5, which further result in cell cycle arrest and apoptosis. VER-49009 inhibits the cell proliferation, and induces G2 phase arrest in hepatic stellate cell line CFSC cells, which may suggest a rational approach in the prevention of liver fibrosis.


    Kinase Assay: Binding of HSP90 inhibitors to human full-length recombinant HSP90β is determined by a competitive binding fluorescence polarization assay, using a fluorescent pyrazole resorcinol probe.


    Cell Assay:  Antiproliferative effects are measured using the sulforhodamine B assay. HUVEC sensitivity is determined by an alkaline phosphatase method. Cells: Melanoma cells (SKMEL 2, SKMEL 5, SKMEL 28, WM266.4); Colon cancer cells (HCT116, BEneg, BE2, HT29, HT29oxaliR); Ovarian cancer cells (CH1, CH1doxR); Breast cancer cells (MB-231, MB-468, BT20, ZR751, MCF7, BT-474); nontumorigenic cells (HUVEC, MCF10a, PNT)

    In VivoIn athymic mice, VER-49009 (20 mg/kg, i.v.) shows rapid clearance with values of 0.187 L/h. In an orthotopic human ovarian carcinoma model, VER-49009 (4 mg/kg, i.p.) also induces the depletion of the sensitive HSP90 client protein ERBB2.
    Animal modelMice bearing established OVCAR3 human ovarian xenografts.
    Formulation & DosageDissolved in 10% DMSO, 5% Tween 20, 85% saline; 4 mg/kg; i.p. injection 
    References

    Mol Cancer Ther. 2007 Apr;6(4):1198-211; Mol Cell Biochem. 2009 Oct;330(1-2):181-5. 


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

    VER-49009

    Pymol diagrams showing binding interactions between the ATP-binding site of human HSP90α and (A) VER-49009 and (B) VER-50589. Mol Cancer Ther. 2007 Apr;6(4):1198-211.

    VER-49009

    Effects of VER-49009 and VER-50589 on molecular biomarkers and apoptosis.


    VER-49009

    Pharmacokinetics of VER-49009 and VER-50589. Mol Cancer Ther. 2007 Apr;6(4):1198-211.

     


    VER-49009

    Effects of VER-49009 and VER-50589 on HSP72 induction and client protein depletion in vivo. Mol Cancer Ther. 2007 Apr;6(4):1198-211.


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