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    NPS-1034
    NPS-1034

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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 #: V0595
    CAS #: 1221713-92-3Purity ≥98%

    Description: NPS-1034 (NPS1034; NPS 1034) is a novel, potent dual inhibitor of the tyrosine kinases Met and Axl with potential antineoplastic activity. It inhibits Met and Axl with IC50s of 48 nM and 10.3 nM, respectively. NPS-1034 shows potent anti-proliferative activity in vitro against cells expressing MET and and high in vivo antitumor efficacy by promoting the regression of tumors in a mouse xenograft  via anti-angiogenic & pro-apoptotic actions. 

    References: Cancer Res. 2014 Jan 1;74(1):253-62; Invest New Drugs. 2014 Jun;32(3):389-99. 

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    Molecular Weight (MW)551.54
    FormulaC31H23F2N5O3
    CAS No.1221713-92-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (181.3 mM)
    Water: <1 mg/mL
    Ethanol: 4 mg/mL (7.3 mM) 
    Solubility (In vivo)PBS: 11mg/mL
    SynonymsNPS-1034; NPS 1034; NPS1034;  

    Chemical Name: N-(3-fluoro-4-((3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxamide.

    InChi Key: RGAZVGZUBCFHRJ-UHFFFAOYSA-N

    InChi Code: InChI=1S/C31H23F2N5O3/c1-18-27(31(40)38(37(18)2)22-11-8-20(32)9-12-22)30(39)36-21-10-13-25(24(33)16-21)41-26-14-15-34-29-28(26)23(17-35-29)19-6-4-3-5-7-19/h3-17H,1-2H3,(H,34,35)(H,36,39)

    SMILES Code: O=C(C1=C(C)N(C)N(C2=CC=C(F)C=C2)C1=O)NC3=CC=C(OC4=C5C(NC=C5C6=CC=CC=C6)=NC=C4)C(F)=C3


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    In Vitro

    In vitro activity: In HCC827/GR cells, NPS-1034 does not show significant antiproliferative effects, while overcomes gefitinib resistance by inhibiting the phosphorylation of MET, Akt, and Erk. In H820 cells, NPS-1034 enhances sensitivity to EGFR-TKIs. In HCC78 cells, NPS-1034 inhibits ROS1 activity and cell proliferation. In addition, a combination of gefitinib and NPS-1034 enhances cell death by inducing caspase-3 and PARP-1 cleavage. NPS-1034 inhibits the viability of the MKN45 and SNU638 cell lines, which highly express the MET gene and p-MET, with IC50 of 112.7 and 190.3 nmol, respectively.


    Kinase Assay: The in vitro NPS-1034 profile of inhibition of RTKs is analyzed using RTK assay kits according to the manufacturer's protocols.


    Cell Assay:  To perform the MTT assay, cells (0.5 × 104/well, HCC827/GR, HCC-78 and H820 cells) are plated in 96-well sterile plastic plates and allowed to attach overnight. Cells are exposed to varying doses of gefitinib, erlotinib, PHA-665752, and NPS-1034 in medium containing 1% FBS. After 72 hours, 15 μL of MTT solution (5 mg/mL) is added to each well and plates are incubated for 4 hours. Crystalline formazan is solubilized with 100 μL of a 10% (w/v) SDS solution for 24 hours. Absorbance at 595 nm is read spectrophotometrically using a microplate reader.

    In VivoIn SCID mice bearing HCC827/GR tumor xenografts, NPS-1034 (10 mg/kg, p.o.) decreases tumor growth, and the combination of gefitinib and NPS-1034 results in enhanced tumor growth inhibition via the inhibition of tumor proliferation and the induction of apoptosis. In nude mice bearing MKN45 xenograft tumors, NPS-1034 (30 mg/kg, p.o.) decreases tumor growth through the inhibition of angiogenesis and the promotion of apoptosis.
    Animal modelSCID mice bearing HCC827/GR tumor xenografts
    Formulation & DosageDissolved in PBS; 10 mg/kg; oral gavage
    References

    Cancer Res. 2014 Jan 1;74(1):253-62; Invest New Drugs. 2014 Jun;32(3):389-99. 


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

    NPS-1034

    Effects of combined treatment with gefitinib and NPS-1034 in HCC827/GR cells with MET gene amplification. Cancer Res. 2014 Jan 1;74(1):253-62.

    NPS-1034

    Effects of combined treatment with erlotinib and NPS-1034 in HCC827/ER cells with AXL activation. Cancer Res. 2014 Jan 1;74(1):253-62.

    NPS-1034

    NPS-1034 treatment inhibited ROS1 activity. A, HCC-78 cells treated with the indicated doses of crizotinib or NPS-1034 for 72 hours. The viability of cells was determined using the MTT assay. B, cells treated with or without the indicated doses of crizotinib or NPS-1034 for 24 hours. Changes in ROS, Akt, and Erk activity and cleaved PARP were analyzed by Western blotting. Cancer Res. 2014 Jan 1;74(1):253-62.


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