Tepotinib (EMD 1214063)

For research use only.

Catalog No.S7067 Synonyms: MSC2156119

8 publications

Tepotinib (EMD 1214063) Chemical Structure

CAS No. 1100598-32-0

Tepotinib (EMD 1214063, MSC2156119) 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. Tepotinib (EMD 1214063) induces autophagy. Phase 1.

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Selleck's Tepotinib (EMD 1214063) has been cited by 8 publications

3 Customer Reviews

  • Ectopic expression of a RNAi-resistant SMARCE1 cDNA resensitizes SMARCE1-knockdown cells to MET inhibition in MET-amplified NSCLC cells. The above-described cells were grown in the absence or presence of 300 nM Crizotinib, 150 nM EMD1214063, or 150 nM PHA665752. Cells were then fixed, stained and photographed after 12 days (untreated) or 28 days (treated).

    Cell Research, 2015, 25: 445-458. Tepotinib (EMD 1214063) purchased from Selleck.

    HCC827 and PC9 cells cultured with CAF-CM were treated with c-met inhibitor Tepotinib (100 nM) or/and IGF1R inhibitor NVP-AEW541 (2 μM), protein expression was determined by western blot. *P<0.05

    Biochim Biophys Acta Mol Basis Dis, 2018, 1864(3):793-803. Tepotinib (EMD 1214063) purchased from Selleck.

  • Anti-viral activity of the kinase inhibitor EMD 1214063. (A) Inhibition of different viruses with EMD 1214063. Monolayers of A549 cells were pre-treated with the indicated concentration of EMD 1214063 for 30 min, followed by infection with the different viruses (MOI = 0.3) in presence of drug. After 1 h, cells were washed with medium containing 20 mM ammonium chloride. Infection o 1212 f rLCMV-LASVGP and LCMV were detected after 16 h by IFA as in (2B). IAV infection was assessed after 6 h by staining for IAV N protein, whereas AdV was detected via its EGFP reporter in direct fluorescence after 24 h (means + SD, n = 3). (B) Representative images of inhibition experiments. LCMV and IAV antigens are in red, EGFP in green, nuclei are stained with DAPI (blue), bar = 100 μM. (C) Anti-viral effect of EMD 1214063 in primary human respiratory epithelial cells. Monolayers of primary human bronchiolar epithelial cells isolated from human bronchi were cultured in M96 plates for four days to obtain closed monolayers. Cells were pre-treated with the indicated concentration of EMD 1214063 for 30 min, followed by infection with rLCMV-LASVGP (LASV) and rLCMV-VSVG (VSV) at 1000 PFU/well for 1 h. Cells were washed and infection detected by IFA after 16 hours as in (2B). Data are means + SD, n = 3.

    J Virol, 2016, 90(14):6412-29. . Tepotinib (EMD 1214063) purchased from Selleck.

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Biological Activity

Description Tepotinib (EMD 1214063, MSC2156119) 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. Tepotinib (EMD 1214063) induces autophagy. Phase 1.
Targets
c-Met [1]
(Cell-free assay)
4 nM
In vitro

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. [1]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A549 cells MU\GeY5kfGmxbjDhd5NigQ>? MU[0OUBucW6| NGPhcmdKdmirYnn0bY9vKG:oIHOtUYV1KGurbnHz[UBqdiCqdX3hckBCPTR7IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YheGixc4Doc5J6dGG2aX;uJIFnfGW{IES1JI1qdnNiYomg[Yxm[3S{b3Po[Y1qdHWvaX7ld4NmdmOnIHHzd4F6NCCLQ{WwQVEzKG6P NWqyfYZiOjV5M{[5PVg>

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-Met / Met / p-ERK / ERK / p-AKT / AKT ; 

PubMed: 26006023     


Western blot analysis monitored decreasing Met, AKT, and Erk1/2 activity levels in Lipo246 cells with increasing concentrations of EMD1214063 (4 h; 10%-FBS containing media).

26006023
Growth inhibition assay
Cell viability; 

PubMed: 26006023     


Left Panel: Lipo246; Right panel: Lipo224. MTS assays measured proliferation rates as a consequence of increasing EMD1214063 treatment (n=3 experiments ± SEM; t-test: *=P<0.05, **=P<0.005, ***=P<0.0001; samples were analyzed at least in duplicate per experiment).

26006023
In vivo EMD 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. [1]

Protocol

Animal Research:

[1]
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  • Animal Models: Human gastric carcinoma xenografts Hs746T
  • Dosages: 15 mg/kg
  • Administration: daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 5 mg/mL warmed (10.15 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing. 		2mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 492.57
Formula

C29H28N6O2
CAS No. 1100598-32-0
Storage powder
in solvent
Synonyms MSC2156119
Smiles CN1CCC(CC1)COC2=CN=C(N=C2)C3=CC=CC(=C3)CN4C(=O)C=CC(=N4)C5=CC=CC(=C5)C#N

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04204902 Completed Drug: Tepotinib 100 mg|Drug: Tepotinib 250 mg Healthy Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany October 17 2019 Phase 1
NCT03940703 Recruiting Drug: Tepotinib|Drug: Osimertinib Non-small Cell Lung Cancer EMD Serono Research & Development Institute Inc.|Merck KGaA Darmstadt Germany|EMD Serono September 19 2019 Phase 2
NCT03629223 Completed Drug: Tepotinib TF2|Drug: Tepotinib TF3 Healthy Merck KGaA Darmstadt Germany August 23 2018 Phase 1
NCT03546608 Completed Drug: Tepotinib Hepatic Impairment EMD Serono Research & Development Institute Inc.|Merck KGaA Darmstadt Germany|EMD Serono June 13 2018 Phase 1
NCT03531762 Completed Drug: Tepotinib|Drug: Omeprazole Healthy Merck KGaA Darmstadt Germany May 14 2018 Phase 1

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c-Met Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID