Tepotinib

Catalog No.S7067 Batch:S706705

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Technical Data

Formula

C29H28N6O2
Molecular Weight 492.57 CAS No. 1100598-32-0
Solubility (25°C)* In vitro DMSO 17 mg/mL (34.51 mM)
Ethanol 6 mg/mL (12.18 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 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]
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 (from reference)

Animal Study:

[1]
  • Animal Models

    Human gastric carcinoma xenografts Hs746T

  • Dosages

    15 mg/kg

  • Administration

    daily

References

  • https://pubmed.ncbi.nlm.nih.gov/23553846/

Customer Product Validation

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).

Data from [ , , Cell Research, 2015, 25: 445-458 ]

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

Data from [ , , Biochim Biophys Acta Mol Basis Dis, 2018, 1864(3):793-803 ]

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.

Data from [ , , J Virol, 2016, 90(14):6412-29. ]

Selleck's Tepotinib has been cited by 22 publications

Efficacy of amivantamab, a bi-specific antibody targeting EGFR and MET, in ALK-rearranged non-small-cell lung cancer cell lines [ Lung Cancer, 2025, 201:108415] PubMed: 39922174
TWIST1 is a critical downstream target of the HGF/MET pathway and is required for MET driven acquired resistance in oncogene driven lung cancer [ Oncogene, 2024, 10.1038/s41388-024-02987-5] PubMed: 38485737
Comparison of Tepotinib, Paclitaxel, or Ramucirumab Efficacy According to the Copy Number or Phosphorylation Status of the MET Gene: Doublet Treatment versus Single Agent Treatment [ Int J Mol Sci, 2024, 25(3)1769] PubMed: 38339049
Comparison of Tepotinib, Paclitaxel, or Ramucirumab Efficacy According to the Copy Number or Phosphorylation Status of the MET Gene: Doublet Treatment versus Single Agent Treatment [ Int J Mol Sci, 2024, 25(3)1769] PubMed: 38339049
Bladder cancer organoids as a functional system to model different disease stages and therapy response [ Nat Commun, 2023, 14(1):2214] PubMed: 37072390
Bladder cancer organoids as a functional system to model different disease stages and therapy response [ Nat Commun, 2023, 14(1):2214] PubMed: 37072390
Suppression of TNBC metastasis by doxazosin, a novel dual inhibitor of c-MET/EGFR [ J Exp Clin Cancer Res, 2023, 10.1186/s13046-023-02866-z] PubMed: 37924112
"Proteotranscriptomic analysis of advanced colorectal cancer patient derived organoids for drug sensitivity prediction" [ J Exp Clin Cancer Res, 2023, 42(1):8] PubMed: 36604765
Efficacy of gilteritinib in comparison with alectinib for the treatment of ALK-rearranged non-small cell lung cancer [ Cancer Sci, 2023, 10.1111/cas.15958] PubMed: 37715310
Responses to the Tepotinib in Gastric Cancers with MET Amplification or MET Exon 14 Skipping Mutations and High Expression of Both PD-L1 and CD44 [ Cancers (Basel), 2022, 14(14)3444] PubMed: 35884507

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SHIPPING AND STORAGE
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