Tepotinib (hydrochloride)

Tepotinib (EMD-1214063) hydrochloride is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib hydrochloride inhibits c-Met phosphorylation and induces autophagy. Tepotinib hydrochloride has antitumor effects[1][2][3].

Product Specifications

CAS Number

[1103508-80-0]

Product Name Alternative

EMD-1214063 (hydrochloride)

UNSPSC

12352005

Target

Autophagy; c-Met/HGFR

Type

Reference compound

Related Pathways

Autophagy; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/tepotinib-hydrochloride.html

Solubility

10 mM in DMSO

Smiles

N#CC1=CC=CC(C(C=CC2=O)=NN2CC3=CC=CC(C4=NC=C(C=N4)OCC5CCN(CC5)C)=C3)=C1.[H]Cl.[x]

Molecular Formula

C29H28N6O2.xHCl

Molecular Weight

492.57 (free base)

References & Citations

[1]Bladt F, et al. EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-Met inhibitors. Clin Cancer Res, 2013, 19 (11), 2941-2951.|[2]A. Naing, et al. IS4-1 - A Phase I Dose-Escalation Study of emd 1214063, an Oral Selective CMET Inhibitor, in Patients with Advanced Solid Tumors. Annals of Oncology. Volume 23, Supplement 11, October 2012, Page xi21.|[3]Zhan N, et al. The Effect of Selective c-MET Inhibitor on Hepatocellular Carcinoma in the MET-Active, β-Catenin-Mutated Mouse Model. Gene Expr. 2018 May 18;18 (2) :135-147.