MK-2461

MK-2461

CAT N°: 32964
Price:

From 276.00 234.60

MK-2461 is an inhibitor of wild-type and mutant forms of c-MET (IC50s = 0.4-2 nM).{61218} It is selective for c-MET over a panel of 13 additional kinases (IC50s = 22-7,800 nM) but does inhibit Ron and FLT1 (IC50s = 7 and 10 nM, respectively). MK-2461 also inhibits autophosphorylation of FGFR2 and PDGFR? in KATO III cells but not EGF-induced phosphorylation of EGFR in A549 lung cancer cells when used at a concentration of 2 µM.{61219} It reduces proliferation in a panel of cancer cell lines, including cells expressing constitutively active c-MET, FGFR2, or PDGFR (IC50s = ?1 µM for all).{61219} MKT-2461 (10-200 mg/kg) reduces tumor growth in a GTL-16 gastric cancer mouse xenograft model.{61218}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N?-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-sulfamide
  • Correlated keywords
    • 1196681-15-8 MK2461 cMET FLT 1 FGFR 2 A 549 GTL16
  • Product Overview:
    MK-2461 is an inhibitor of wild-type and mutant forms of c-MET (IC50s = 0.4-2 nM).{61218} It is selective for c-MET over a panel of 13 additional kinases (IC50s = 22-7,800 nM) but does inhibit Ron and FLT1 (IC50s = 7 and 10 nM, respectively). MK-2461 also inhibits autophosphorylation of FGFR2 and PDGFR? in KATO III cells but not EGF-induced phosphorylation of EGFR in A549 lung cancer cells when used at a concentration of 2 µM.{61219} It reduces proliferation in a panel of cancer cell lines, including cells expressing constitutively active c-MET, FGFR2, or PDGFR (IC50s = ?1 µM for all).{61219} MKT-2461 (10-200 mg/kg) reduces tumor growth in a GTL-16 gastric cancer mouse xenograft model.{61218}

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