TRK-IN-34 is an orally active TRK and TRKC mutant kinase inhibitor, with IC 50 values of 0.75 nM and 0.96 nM against TRKA G595R and TRKA G667C , respectively. TRK-IN-34 inhibits the kinase activities of TRKA G595R and TRKA G667C at the functional level. TRK-IN-34 inhibits the proliferation of TRKA-transfected cells, exerts tumor growth-inhibitory effects and achieves partial tumor regression in xenograft models. TRK-IN-34 can be used to study TRK inhibitor-resistant cancers driven by the TRKA G667C mutation.
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