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. Author manuscript; available in PMC: 2018 Jan 1.

Published in final edited form as: Clin Cancer Res. 2016 Jul 1;23(1):204–213. doi: 10.1158/1078-0432.CCR-15-1601

A: Inhibition of Ba/F3 transformed with CD74-ROS1 wildtype (red, ), G2032R (green, ), L2026M (blue, ), and Ba/F3 parental cells (black, ●). B: Effect of drugs on ROS1 autophosphorylation (pY2274) and downstream activation of ERK signaling. C: Inhibition of the HCC78 NSCLC cell line by brigatinib (blue, , IC₅₀ = 2.2 μM), cabozantinib (red, , IC₅₀ = 1.36 μM) crizotinib (green, , IC₅₀ = 1.6 μM), and foretinib (black, ●, IC₅₀ = 0.46 μM); data for alectinib (IC₅₀ = 0.75 μM), brigatinib (IC₅₀ = 2.2 μM), ceritinib (IC₅₀ = 0.53 μM), entrectinib (IC₅₀ = 0.45 μM), and PF-06463922 (IC₅₀ = > 10 μM) not shown. D: Inhibition of ROS signaling in HCC78 cells. E: Molecular modeling of cabozantinib into the active site of ROS1 kinase domain, with dashed lines indicating hydrogen bonds.

Inline graphic — A: Inhibition of Ba/F3 transformed with CD74-ROS1 wildtype (red, ), G2032R (green, ), L2026M (blue, ), and Ba/F3 parental cells (black, ●). B: Effect of drugs on ROS1 autophosphorylation (pY2274) and downstream activation of ERK signaling. C: Inhibition of the HCC78 NSCLC cell line by brigatinib (blue, , IC₅₀ = 2.2 μM), cabozantinib (red, , IC₅₀ = 1.36 μM) crizotinib (green, , IC₅₀ = 1.6 μM), and foretinib (black, ●, IC₅₀ = 0.46 μM); data for alectinib (IC₅₀ = 0.75 μM), brigatinib (IC₅₀ = 2.2 μM), ceritinib (IC₅₀ = 0.53 μM), entrectinib (IC₅₀ = 0.45 μM), and PF-06463922 (IC₅₀ = > 10 μM) not shown. D: Inhibition of ROS signaling in HCC78 cells. E: Molecular modeling of cabozantinib into the active site of ROS1 kinase domain, with dashed lines indicating hydrogen bonds.