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    HSP990 (NVP-HSP990)
    HSP990 (NVP-HSP990)

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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 #: V0881
    CAS #: 934343-74-5Purity ≥98%

    Description: NVP-HSP990 (NVP HSP 990; NVP-HSP-990; HSP990; HSP-990) is an orally bioavailable HSP90 (heat shock protein 90) inhibitor with potential antitumor activity. It inhibits HSP90α/β with IC50s of 0.6 nM/0.8 nM. NVP-HSP990 exhibits low nanomolar (single digit IC50 values) activity against various Hsp90 isoforms (Hsp90α, Hsp90β, and GRP94) and high selectivity over unrelated enzymes, receptors, and kinases.

    References: Mol Cancer Ther. 2012 Mar;11(3):730-9; Cancer Res. 2013 May 15;73(10):3062-74.

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    Molecular Weight (MW)379.39
    FormulaC20H18FN5O2
    CAS No.934343-74-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 75 mg/mL (197.7 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)Chemical Name: (R)-2-amino-7-(4-fluoro-2-(6-methoxypyridin-2-yl)phenyl)-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one
    InChi Key: WSMQUUGTQYPVPD-OAHLLOKOSA-N
    InChi Code: InChI=1S/C20H18FN5O2/c1-10-18-16(26-20(22)23-10)9-15(25-19(18)27)12-7-6-11(21)8-13(12)14-4-3-5-17(24-14)28-2/h3-8,15H,9H2,1-2H3,(H,25,27)(H2,22,23,26)/t15-/m1/s1
    SMILES Code: O=C1N[[email protected]@H](C2=CC=C(F)C=C2C3=NC(OC)=CC=C3)CC4=NC(N)=NC(C)=C41
    SynonymsNVP HSP 990; NVP-HSP990; HSP990; HSP-990; HSP 990; NVP HSP-990


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    In Vitro

    In vitro activity: NVP-HSP990 is based on a 2-amino-4-methyl-7,8-dihydropyrido[4,3-d]pyrimidin-5(6H)-one scaffold, which is structurally distinct from other known HSP90 inhibitors. NVP-HSP990 binds to the N-terminal ATP-binding domain of HSP90. NVP-HSP990 exhibits single digit nanomolar IC50 values on three of the HSP90 isoforms (HSP90α, HSP90β, and GRP94) and 320 nM IC50 value on the fourth (TRAP-1), with selectivity against unrelated enzymes, receptors, and kinases. NVP-HSP990 dissociates the HSP90-p23 complex, depleted client protein c-Met, and induced Hsp70 in c-Met amplified GTL-16 gastric tumor cells. NVP-HSP990 potently inhibites the growth of human cell lines and primary patient samples from a variety of tumor types. NVP-HSP990 displays dose- and time-dependent effects on HSP90 client proteins. NVP-HSP990 inhibits Glioma tumor-initiating cells (GIC) proliferation in all GIC lines, with IC50 values ranging approximately between 10 and 500 nM. Olig2 is a functional marker associated with cell proliferation and response to NVP-HSP990, as NVP-HSP990 attenuated cell proliferation in Olig2-high GIC lines. In addition, NVP-HSP990 disrupted cell-cycle control mechanism by decreasing CDK2 and CDK4 and elevating apoptosis-related molecules.


    Kinase Assay: The potency of HSP90 inhibitors for HSP90α, HSP90β, and Grp94 is determined by AlphaScreen competition binding assays, and activity against TRAP-1 is assessed by an ATPase assay.


    Cell Assay: Dissociated GICs are plated at 10 cells/μL in 6-well plates and incubated with various concentrations of NVP-HSP990 for 7 days. Formed tumorspheres are dissociated into single cells and counted with hemocytometer using 0.2% Trypan blue exclusion.

    In VivoNVP-HSP990 exhibits drug-like pharmaceutical and pharmacologic properties with high oral bioavailability. In the GTL-16 xenograft model, a single oral administration of 15 mg/kg of NVP-HSP990 induced sustained downregulation of c-Met and upregulation of Hsp70. In repeat dosing studies, NVP-HSP990 treatment resulted in tumor growth inhibition of GTL-16 and other human tumor xenograft models driven by well-defined oncogenic HSP90 client proteins.
    Animal modelGTL-16, NCI-H1975, BT474, and MV4;11 tumor xenografted nude and SCID mice models
    Formulation & DosageDissolved in 100% polyethylene glycol (PEG400); 15 mg/kg; oral gavage
    References

    Mol Cancer Ther. 2012 Mar;11(3):730-9; Cancer Res. 2013 May 15;73(10):3062-74.


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

    HSP990 (NVP-HSP990)

    Chemical structure (A) and cellular activity (B–D) of NVP-HSP990. B, in vitro effects of NVP-HSP990 on p23-Hsp90 complex. Mol Cancer Ther. 2012 Mar;11(3):730-9.
     

    HSP990 (NVP-HSP990)

    Pharmacokinetic–pharmacodynamic relationship of various Hsp90 inhibitors in vivo. Mol Cancer Ther. 2012 Mar;11(3):730-9.
     

    HSP990 (NVP-HSP990)

    Efficacy and pharmacodynamics of NVP-HSP990 in BT-474 and MV4;11 tumor models. Mol Cancer Ther. 2012 Mar;11(3):730-9.
     

    HSP990 (NVP-HSP990)

    Efficacy and pharmacodynamics of NVP-HSP990 in GTL-16 tumor model. Mol Cancer Ther. 2012 Mar;11(3):730-9.
     

    HSP990 (NVP-HSP990)

    Efficacy and pharmacodynamics of NVP-HSP990 in H1975 and A549 tumor models. Mol Cancer Ther. 2012 Mar;11(3):730-9. 


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