Tepotinib

• Description:

  Tepotinib (EMD-1214063) 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 inhibits c-Met phosphorylation and induces autophagy. Tepotinib has antitumor effects[1][2][3].

• Product Name Alternative:

  EMD-1214063

• UNSPSC:

  12352005

• Hazard Statement:

  H315, H319, H320

• 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/EMD-1214063.html

• Purity:

  99.94

• Solubility:

  DMSO : 8.75 mg/mL (ultrasonic; warming; heat to 60°C)

• Smiles:

  N#CC1=CC=CC(C(C=CC2=O)=NN2CC3=CC=CC(C4=NC=C(C=N4)OCC5CCN(CC5)C)=C3)=C1

• Molecular Formula:

  C29H28N6O2

• Molecular Weight:

  492.57

• Precautions:

  H315, H319, H320

• 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]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.|[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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• CAS Number:

  [1100598-32-0]