Home Protein Tyrosine Kinase c-Met inhibitor - Autophagy activator Tepotinib For research use only.

Tepotinib

Synonyms: EMD 1214063, MSC2156119

Tepotinib 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.

Tepotinib Chemical Structure

Tepotinib Chemical Structure

CAS No. 1100598-32-0

Purity & Quality Control

Tepotinib Related Products

Signaling Pathway

c-Met Signaling Pathways

c-Met Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 Function assay 45 mins Inhibition of c-Met kinase in human A549 cells assessed as inhibition of phosphorylation after 45 mins by electrochemiluminescence assay, IC50=0.012μM 25736998
EBC1 Antitumor assay 15 mg/kg 5 days Antitumor activity against human EBC1 cells xenografted in CD-1 nude mouse assessed as tumor regression at 15 mg/kg, po qd administered for 5 days on and 2 days off up to 32 days 25736998
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
Click to View More Cell Line Experimental Data

Biological Activity

Description Tepotinib 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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-Met / Met / p-ERK / ERK / p-AKT / AKT 26006023
Growth inhibition assay Cell viability 26006023
In Vivo
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]
Animal Research Animal Models Human gastric carcinoma xenografts Hs746T
Dosages 15 mg/kg
Administration daily
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05782361 Recruiting
Advanced Cancer|Non Small Cell Lung Cancer
Institute of Cancer Research United Kingdom|Merck Serono GmbH Germany|Merck Sharp & Dohme LLC
 May 3 2023 Phase 1
NCT05120960 Withdrawn
Brain Tumor
M.D. Anderson Cancer Center
 February 27 2023 Phase 1
NCT04739358 Terminated
Advanced Non-Small Cell Lung Cancer With MET Mutations
Criterium Inc.|EMD Serono Research & Development Institute Inc.
 May 25 2022 Phase 1|Phase 2
NCT05203822 Completed
Healthy
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany
 January 21 2022 Phase 1
NCT05213481 Completed
Healthy
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany
 December 15 2021 Phase 1
NCT04204902 Completed
Healthy
Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany
 October 17 2019 Phase 1

Chemical Information & Solubility

Molecular Weight 492.57 Formula

C29H28N6O2
CAS No. 1100598-32-0 SDF Download Tepotinib SDF
Smiles CN1CCC(CC1)COC2=CN=C(N=C2)C3=CC=CC(=C3)CN4C(=O)C=CC(=N4)C5=CC=CC(=C5)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 17 mg/mL ( (34.51 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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Tech Support

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