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Fig. 1 | BMC Cancer

Fig. 1

From: Discovery of a novel ALK/ROS1/FAK inhibitor, APG-2449, in preclinical non-small cell lung cancer and ovarian cancer models

Fig. 1

APG-2449 exhibits potent inhibitory activity against ALK/ROS1/FAK kinases and proliferation of relevant cell lines. A, Chemical structure of APG-2449. B, Dissociation constants (Kd values, nM) of APG-2449 calculated from KINOMEscan®. C, TREEspot interaction map of KINOMEscan selectivity panel for APG-2449 at 100 nM. Red spheres: kinases inhibited to < 35% of controls. Circle size reflects binding affinity. D, Inhibition of wild-type (wt) ALK and ALK mutants by APG-2449 and second-generation ALK inhibitors alectinib and ceritinib, using LANCE TR-FRET assay (IC50). E, Antiproliferative activity of APG-2449 (log IC50) in a panel of cancer cell lines. Data represent the mean of at least 2 independent experiments performed with triplicates. LANCE TR-FRET, lanthanide chelate excite time-resolved fluorescence resonance energy transfer

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