Tepotinib | Selective c-MET inhibitor
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $60.00 | ||
| 25 mg | $200.00 |
Tepotinib (1100598-32-0) 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.
References/Citations:
- Albers et al. (2023), The Preclinical Pharmacology of Tepotinib – A Highly Selective MET Inhibitor with Activity in Tumors Harboring MET Alterations; Mol. Cancer Ther. 22 833
- Bladt et al. (2013), EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-MET inhibitors; Clin. Cancer Res. 19 2941
- Friese-Hamim et al. (2022), Brain penetration and efficacy of tepotinib in orthotopic patient-derived xenograft models of MET-driven non-small cell lung cancer in brain metastases; Lung Cancer 163 77
- Friese-Hamim et al. (2017), The selective c-MET inhibitor tepotinib can overcome epidermal growth factor receptor inhibitor resistance mediated by aberrant c-MET activation in NSCLC models; Am. J. Cancer Res. 7 962
C29H28N6O2
>98% TLC
NMR: (Conforms)
Safety Data Sheet:
Product Data Sheet:
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Tepotinib (1100598-32-0) 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.
References/Citations:
- Albers et al. (2023), The Preclinical Pharmacology of Tepotinib – A Highly Selective MET Inhibitor with Activity in Tumors Harboring MET Alterations; Mol. Cancer Ther. 22 833
- Bladt et al. (2013), EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-MET inhibitors; Clin. Cancer Res. 19 2941
- Friese-Hamim et al. (2022), Brain penetration and efficacy of tepotinib in orthotopic patient-derived xenograft models of MET-driven non-small cell lung cancer in brain metastases; Lung Cancer 163 77
- Friese-Hamim et al. (2017), The selective c-MET inhibitor tepotinib can overcome epidermal growth factor receptor inhibitor resistance mediated by aberrant c-MET activation in NSCLC models; Am. J. Cancer Res. 7 962
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