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    Tepotinib (EMD 1214063; MSC 2156119)
    Tepotinib (EMD 1214063; MSC 2156119)

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    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0596
    CAS #: 1100598-32-0Purity ≥98%

    Description: This product has been discontinued. Tepotinib (formerly EMD 1214063, EMD-1214063; MSC2156119; MSC-2156119; Tepmetko) is a selective c-Met inhibitor with potential antineoplastic activity. Tepotinib has been approved in 2020 in Japan and in the USA in 2021 for the treatment of adults with metastatic non-small cell lung cancer whose tumors have a mutation that leads to mesenchymal-epithelial transition exon 14 skipping. It inhibits c-Met with an IC50 of 4 nM, and is >200-fold selective for inhibiting c-Met over other kinases such as IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib can inhibit HGF-induced c-Met phosphorylation with an average IC50 of 6 nM in A549 cells. It also significantly inhibits the activation of downstream signaling pathways of c-Met including the phosphorylation of Akt, Gab-1and Erk1/2.

    References: Clin Cancer Res. 2013 Jun 1;19(11):2941-51.

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    Molecular Weight (MW)492.57
    CAS No.1100598-32-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 5 mg/mL (10.2 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)5% DMSO+corn oil: 5mg/mL
    SynonymsEMD-1214063, MSC-2156119; EMD1214063; EMD 1214063; MSC2156119; MSC 2156119; Tepotinib.

    IUPAC/Chemical Name: 3-(1-(3-(5-((1-methylpiperidin-4-yl)methoxy)pyrimidin-2-yl)benzyl)-1,6-dihydro-6-oxopyridazin-3-yl)benzonitrile


    InChi Code: InChI=1S/C29H28N6O2/c1-34-12-10-21(11-13-34)20-37-26-17-31-29(32-18-26)25-7-3-5-23(15-25)19-35-28(36)9-8-27(33-35)24-6-2-4-22(14-24)16-30/h2-9,14-15,17-18,21H,10-13,19-20H2,1H3

    SMILES Code: N#CC1=CC=CC(C(C=C2)=NN(CC3=CC=CC(C4=NC=C(OCC5CCN(C)CC5)C=N4)=C3)C2=O)=C1

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    In Vitro

    In vitro activity: EMD 1214063 inhibits HGF-induced c-Met phosphorylation in A549 cells with IC50 of 6 nM. Treatment with EMD 1214063 induces a marked reduction of c-Met–constitutive phosphorylation in EBC-1 cells with IC50 of 9 nM. EMD 1214063 effectively blocka phosphorylation of the major downstream effectors of the c-Met enzyme, such as Grb2, Gab1, Sos, PLCγ, and phosphoinositide 3-kinase, in EBC-1, MKN-45, and Hs746T cells in the range of 1 to 10 nM. EMD 1214063 considerably inhibits the viability of MKN-45 cells with IC50 of less than 1 nM. Treatment with EMD 1214063 (as low as 0.1 nM) inhibits HGF-induced NCI-H441 cell migration, whereas concentrations of 100 nM to 1 μM almost completely prevents it.

    Kinase Assay: Tepotinib (EMD-1214063) is a potent and selective c-Met inhibitor with IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer.

    In VivoEMD 1214063 treatment, at doses of 10 mg/kg or more, results in more than 90% inhibition of c-Met phosphorylation in Hs746T xenograft tumor for a period of at least 72 hours. EMD 1214063 induces more than 50% reduction of cyclin D1 expression, which persists after 96 hours upon treatment with doses of 100 mg/kg. A transient induction of p27 and cleaved caspase-3 are also observed upon treatment with EMD 1214063. EMD 1214063 (15 mg/kg, daily) treatment induces complete regression of gastric carcinoma xenografts Hs746T, in which c-Met is amplified, overexpressed, and activated in a ligand-independent fashion.
    Animal modelXenografts Hs746T
    Formulation & Dosage15 mg/kg

    Clin Cancer Res. 2013 Jun 1;19(11):2941-51

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

    Tepotinib (EMD 1214063)

    Dose-dependent inhibition of c-Met auto-phosphorylation in vivo. Clin Cancer Res. 2013 Jun 1;19(11):2941-51.

    Tepotinib (EMD 1214063)

    EMD 1214063 and EMD 1204831 effectively inhibit tumor c-Met auto-phosphorylation and cyclin D1 expression while inducing p27 expression. Clin Cancer Res. 2013 Jun 1;19(11):2941-51.

    Tepotinib (EMD 1214063)

    EMD 1214063 and EMD 1204831 display antitumor activity in HGF-dependent and HGF-independent xenograft tumor models. Clin Cancer Res. 2013 Jun 1;19(11):2941-51.


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