CH5424802 is an ATP-competitive inhibitor for ALK and L1196M with Ki values of 0.83 nM and 1.56 nM, respectively. CH5424802 prevents autophosphorylation of ALK, and also suppresses the phosphorylation of STAT3 and AKT, but not of ERK1/2. CH5424802 elicits an apoptotic marker—caspase-3/7-like activation—in NCI-H2228 spheroid cells. CH5424802 blocks the growth of two NPM-ALK expressing lymphoma lines, KARPAS-299 and SR with greater efficacy against KARPAS-299 at an IC50 of 3 nM.
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