Tepotinib (EMD 1214063)

Catalog No.S7067 Synonyms: MSC2156119

Tepotinib (EMD 1214063) Chemical Structure

Molecular Weight(MW): 492.57

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. Phase 1.

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2 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.

    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) 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. 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 NGW1VohHfW6ldHnvckBie3OjeR?= MknOOFUhdWmwcx?= NFS3VJhKdmirYnn0bY9vKG:oIHOtUYV1KGurbnHz[UBqdiCqdX3hckBCPTR7IHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YheGixc4Doc5J6dGG2aX;uJIFnfGW{IES1JI1qdnNiYomg[Yxm[3S{b3Po[Y1qdHWvaX7ld4NmdmOnIHHzd4F6NCCLQ{WwQVEzKG6P MoHjNlU4OzZ7OUi=

... Click to View More Cell Line Experimental Data

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]

+ Expand
  • Animal Models: Human gastric carcinoma xenografts Hs746T
  • Formulation: --
  • 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 individually and in order:
5% DMSO+corn oil
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
Synonyms MSC2156119

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02864992 Recruiting Lung Adenocarcinoma Stage IIIB/IV EMD Serono Research & Development Institute, Inc.|Merck KGaA|EMD Serono September 2016 Phase 2
NCT03021642 Completed Healthy Merck KGaA January 2016 Phase 1
NCT01982955 Recruiting Non-small Cell Lung Cancer Merck KGaA December 2013 Phase 1|Phase 2
NCT01014936 Completed Patients With Solid Tumors, Either Refractory to Standard Therapy or for Which no Effective Standard Therapy is Available EMD Serono|Merck KGaA November 2009 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