现货,pf-k8凯发

pf-04217903 is an orally bioavailabe, small-molecule met tyrosine kinase inhibitor with potential antineoplastic activity. ^[1]
pf-04217903 demonstrates exquisite kinase selectivity. inhibition studies of the c-met mutants show that pf-04217903 is more susceptible to oncogenic mutations that attenuate potency than pf-02341066. ^[1]
pf-04217903 was evaluated against multiple kinase selectivity screening panels: invitrogen inc. (125 kinases), millipore/upstate ltd. (105 kinases), university ofdundee (51 kinases), and pfizer in-house (48 kinases) (supporting information). on the basis of the percent inhibition or ic50 values generated from each of these screens, pf-04217903 was estimated to be>1000-fold selective for c-met compared with each of the other kinases included in these collective screening assays. ^[1]

• enzymatic characterization of c-met receptor tyrosine kinase oncogenic mutants and kinetic studies with aminopyridine and triazolopyrazine inhibitors sergei l. timofeevski, michele a. mctigue, et al. biochemistry 2009;48:5339–5349

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