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    AMG-208
    AMG-208

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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 #: V0599
    CAS #: 1002304-34-8Purity ≥98%

    Description: AMG 208 (AMG-208) is a novel, highly potent and selective triazolopyridazine-based small molecule inhibitor of c-Met with potential antineoplastic activity. It inhibits c-Met with IC50 of 9 nM. MET is an oncogene activated by its ligand, hepatocyte growth factor. Deregulated/disrupted c-Met signaling pathway has been observed in multiple cancer types.

    References: J Med Chem. 2008 May 22;51(10):2879-82; Bioorg Med Chem Lett. 2009 Nov 15;19(22):6307-12. 

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    Molecular Weight (MW)383.4
    FormulaC22H17N5O2
    CAS No.1002304-34-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 0.25 mg/mL (0.65 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL 
    SynonymsAMG 208; AMG-208; AMG208; 4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]-7-methoxyquinoline 

    InChi Key: HEAIZQNMNCHNFD-UHFFFAOYSA-N

    InChi Code: InChI=1S/C22H17N5O2/c1-28-16-7-8-17-19(13-16)23-12-11-20(17)29-14-22-25-24-21-10-9-18(26-27(21)22)15-5-3-2-4-6-15/h2-13H,14H2,1H3

    SMILES Code: COC1=CC=C2C(OCC3=NN=C4C=CC(C5=CC=CC=C5)=NN43)=CC=NC2=C1


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    In Vitro

    In vitro activity: AMG-208 shows the potent inhibition of kinase c-Met activity with IC50 of 9 nM in a cell-free assay. Besides, AMG-208 treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM. Incubation of AMG-208 with rat and human liver microsomes in the presence of NADPH qualitatively yields C6-phenylarene oxidation products as the major metabolites. Pre-incubation of AMG-208 with human liver microsomes for 30 minutes shows a potent time-dependent inhibition for CYP3A4 metabolic activity with IC50 of 4.1 μM, which is an eightfold decrease relative to the IC50 (32 μM) without preincubation. AMG-208 is identified to be a c-MET and RON dual selective inhibitor.


    Kinase Assay: AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.


    Cell Assay: Pre-incubation of AMG-208 with human liver microsomes for 30 minutes shows a potent time-dependent inhibition for CYP3A4 metabolic activity with IC50 of 4.1 μM, which is an eightfold decrease relative to the IC50 (32 μM) without preincubation.

    In VivoIn male Sprague−Dawley rats, AMG-208 (0.5 mg/kg i.v.) shows a high bioavailability with Cl of 0.37 L/h/kg, Vss of 0.38 L/kg and T1/2 of 1 hour, while AMG-208 (2 mg/kg i.v.) shows a bioavailability with AUC0→∞ of 2517 ng·h/mL and F of 43%, respectively.
    Animal modelMale Sprague-Dawley rats
    Formulation & DosageDissolved in DMSO; ≤2 mg/kg; i.v. or p.o.
    ReferencesJ Med Chem. 2008 May 22;51(10):2879-82; Bioorg Med Chem Lett. 2009 Nov 15;19(22):6307-12. 


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

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