Tepotinib

• Background:

  Tepotinib is a selective type 1b MET inhibitor. In biochemical assays using His6-tagged recombinant human MET kinase domain, tepotinib inhibited kinase activity in a concentration-dependent manner with IC50=1.8 nM.1 It displays marked antitumor activity in MET-dependent tumor models.2 It crosses the blood-brain barrier and displays intracranial antitumor activity.3 Tepotinib can overcome EGFR inhibitor resistance mediated by aberrant c-Met activation4 and is in clinical use for non-small cell lung cancer harboring MET exon 14 skipping alterations.

• Conjugation:

  Unconjugated

• Buffer:

  White solid

• Storage Conditions:

  -20°C