Description
PF-04217903, with triazolopyrazine chemical structure, can potently inhibit c-Met with IC50 of 4.8 nM.
Storage
2 years at -20 centigrade
Molecular Formula
C19H16N8O
Chemical Name
2-(4-(3-(quinolin-6-ylmethyl)-3H-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)-1H-pyrazol-1-yl)ethanol
Solubility
DSMO 5 mg/mL Water
In vitro
PF-04217903, with triazolopyrazine chemical structure, can potently inhibit c-Met with IC50 of 4.8 nM. PF-04217903 is a high selective and ATP-competitive inhibitor, and PF-04217903 shows more than 1000-fold selective relative to 208 kinases. PF-04217903 shows inhibition to c-Met-driven processes such as cell growth (proliferation and survival), motility, invasion, and morphology in a variety of tumor cells.
In vivo
Complete inhibition of c-Met activity by PF-04217903 only led to partial tumor growth inhibition (38%-46%) in human xenograft models that express relatively high levels of c-Met. PF-04217903 can potently induce phospho-PDGFRbeta (platelet-derived growth factor receptor) levels in U87MG xenograft tumor.
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