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> Tepotinib [1100598-32-0]

Tepotinib [1100598-32-0]

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Katalog-Nummer 10-5322-5mg

Size : 5mg

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Tepotinib | Selective c-MET inhibitor

CAS:
 1100598-32-0
Catalog Number:
 10-5322

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5 mg$60.00
25 mg$200.00
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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:

  1. 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
  2. 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
  3. 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
  4. 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
CAS:
1100598-32-0
Catalog Number:
10-5322
Activity:
Selective c-MET inhibitor
Chemical Names:
3-(1-(3-(5-((1-Methylpiperidin-4-yl)methoxy)pyrimidin-2-yl)benzyl)-6-oxo-1,6-dihydropyridazin-3-yl)benzonitrile
Alternate Name:
EMD 1214063
Molecular Weight:
492.58
Molecular Formula:

C29H28N6O2

Solubility:
Soluble in DMSO (17 mg/mL with warming)
Physical Properties:
White solid
Purity:

>98% TLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO or water may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

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:

  1. 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
  2. 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
  3. 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
  4. 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