Tepotinib, c-MET inhibitor

Product Details

Formal Name: 3-(1-(3-(5-((1-Methylpiperidin-4-yl)methoxy)pyrimidin-2-yl)benzyl)-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile

Alternate Names: EMD-1214063

Molecular Formula: C₂₉H₂₈N₆O₂

Formula Weight: 492.6

CAS Number: 1100598-32-0

Purity: >98%

Formulation: Powder

Solubility: Soluble in Water (17 mg/ml with warming)

Storage: -20°C

Stability: ≥ 2 years.

Applications

c-MET inhibitor

Functions

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. It displays marked antitumor activity in MET-dependent tumor models. It crosses the blood-brain barrier and displays intracranial antitumor activity. Teptotinib can overcome EGFR inhibitor resistance mediated by aberrant c-Met activation and is in clinical use for non-small cell lung cancer harboring MET exon 14 skipping alterations.

Application Procedures

First dissolved in Water (17 mg/ml), then diluted to aqueous buffer. Solutions in water may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)