Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 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
Purity: ≥98%
Formula Markup: C24H25N5O5S
Formula Weight: 495.552
CAS Number: 917879-39-1
Notes: 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 PDGFRα 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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