Tepotinib hydrochloride  (Synonyms: EMD-1214063 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].

Tepotinib hydrochloride inhibits IRAK4, TrkA, Axl, IRAK1, Mer, and TrkA with IC₅₀s of 615, 1017, 1566, 2037, 2272, and 5716 nM, respectively^[1].
Tepotinib hydrochloride inhibits HGF-induced c-Met phosphorylation, with an average IC₅₀ of 6 nM in A549 cells^[1].
Tepotinib (0.01 nM-30 μM) hydrochloride inhibits tumor cell proliferation and migration in vitro^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tepotinib hydrochloride induces tumor regression in xenograft models and inhibits in vivo c-Met phosphorylation^[1]。

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

492.57 (free base)

C₂₉H₂₈N₆O₂.xHCl

1103508-80-0

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [2]. 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.  [Content Brief]

  [3]. 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.