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    SGX-523
    SGX-523

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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 #: V0593
    CAS #: 1022150-57-7Purity ≥98%

    Description: SGX-523 (SGX 523; SGX523) is a novel, exquisitely selective, and ATP-competitive inhibitor of Hepatocyte growth factor receptor/Met with potential anticancer activity. It inhibits the tyrosine kinase Met with an IC50 of 4 nM, and exhibits no activity against BRAFV599E, c-Raf, Abl and p38α. MET is implicated in the development and progression of various cancer types. 

    References: Mol Cancer Ther. 2009 Dec;8(12):3181-90.

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    Molecular Weight (MW)359.41
    FormulaC18H13N7S
    CAS No.1022150-57-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 3 mg/mL (8.3 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)0.5% methylcellulose+0.2% Tween 80: 30 mg/mL
    SynonymsSGX-523; SGX 523; SGX523;  

    Chemical Name: 6-((6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)thio)quinoline

    SMILES Code: CN1N=CC(C2=NN3C(C=C2)=NN=C3SC4=CC=C5N=CC=CC5=C4)=C1


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    In Vitro

    In vitro activity: SGX-523 belongs to the class of c-Met/hepatocyte growth factor receptor (HGFR) tyrosine kinase inhibitors. SGX-523 stabilizes MET in a unique inactive conformation that is inaccessible to other protein kinases, suggesting an explanation for its selectivity. SGX523 potently inhibits the purified MET catalytic domain but not the closely related receptor tyrosine kinase RON. SGX523 indicates ATP-competitive inhibition with higher apparent affinity for the less active, unphosphorylated form of MET [MET-KD(0P), with a Ki of 2.7 nM] versus the more active phospho-enzyme [MET-KD(3P), with a Ki of 23 nM], a phenomenon consistent with preferential binding to an inactive enzyme conformation. SGX523 inhibits MET-mediated signaling, cell proliferation and cell migration at nanomolar concentrations but had no effect on signaling dependent on other protein kinases, including the closely related RON, even at micromolar concentrations.


    Kinase Assay: Initial rate constants are measured at 21 °C in the presence of 100 mM HEPES (pH 7.5), 0.3 mg/mL poly(Glu-Tyr) peptide substrate, 10 mM MgCl2, 1 mg/mL bovine serum albumin, 5% DMSO, 20 nM MET-KD and various concentrations of ATP and SGX523. Total reaction volumes (20 μL) are quenched with 20 μL Kinase-Glo detection buffer. Luminescence is detected in a plate-reading luminometer and the results are analyzed by nonlinear regression.


    Cell Assay:  MDCK cells are seeded at 1 × 103 per well in a 24-well plate and incubated at 37 °C in 5% CO2 for 1 week in MEM and 10% fetal bovine serum. HGF (90 ng/mL) and various concentrations of SGX523 are added and the cells are incubated for another 18 hours (37 °C, 5% CO2 humidified incubator) and visualized. A549 cells are plated in 12-well plates (6 × 104 per well) and incubated to confluence to investigate cell migration. A channel is introduced into the monolayers by scratching with a pipette tip. Various dilutions of compound are added in starve medium in the presence and absence of HGF (90 ng/mL).The wells are checked for cell migration after twenty-four.

    In Vivo SGX523 significantly retards the growth of preestablished GTL16 tumors when administered orally at doses of ≥10 mg/kg twice daily. SGX523 potently inhibits U87MG tumor growth; at 30 mg/kg dosed twice daily, SGX523 leads to clear regression of U87MG tumors. SGX523, dosed twice daily at 30 mg/kg, also retards the growth of H441 tumors with concomitant reduction in tumor MET autophosphorylation levels. SGX523 inhibition of MET in vivo is associated with the dose-dependent inhibition of growth of tumor xenografts derived from human glioblastoma, lung and gastric cancers, confirming the dependence of these tumors on MET catalytic activity.
    Animal model Harlan nude mice with GTL16, U87, or H441 tumor xenografts
    Formulation & Dosage Formulated in 0.5% MC 400 with 0.05% Tween 80; 60 mg/kg; oral gavage
    References

    Mol Cancer Ther. 2009 Dec;8(12):3181-90.


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

    SGX-523

    SGX-523
    SGX-523


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