Fig. 3: KY216 effectively blocks NSCLC growth in vivo and metastasis in vitro.

a Schematic of the drug administration regimen and representative images of resected tumors from the NCI-H460 xenograft model treated with KY216 (5, 10, or 20 mg/kg) or paclitaxel (10 mg/kg) (n = 6 mice per group). b The tumor volume in nude mice treated with KY216 and paclitaxel is shown, with significance indicated by comparison of tumor volume at day 14 vs day 0 (n = 6 mice per group). c The body weight of xenografted nude mice following treatment with KY216 and paclitaxel, with significance determined by comparing the body weights on Day 14 and Day 0 (n = 6 mice per group). d Immunohistochemical and haematoxylin–eosin (H&E) analysis were shown (n = 6 mice per group). Scale bar: 50 μm. e, f Invasion and migration (e) of NCI-H460 and 95-D cells (independant biological replicates n = 3) and the corresponding protein blot analysis (f) of mesenchymal markers (independant biological replicates n = 3). Scale bar: 50 μm. g, h KY216 decreased TGF-β-induced migration and invasion (g) of NCI-H460 cells (independant biological replicates n = 3). Protein blot analysis (h) was conducted to evaluate the corresponding mesenchymal markers, ZEB1 and p-Smad2 (independant biological replicates n = 3). Scale bar: 50 μm. i–k Treatment with KY216 reduced the migration and invasion abilities (i) of TGF-β-induced NCI-H460 and 95-D cells (independant biological replicates n = 3) and the protein blotting (independant biological replicates n = 3) of epithelial and mesenchymal markers, ZEB1 and p-smad2, in 95-D (j) and TGF-β-induced NCI-H460 cells (k). Scale bar: 50 μm. l Confocal microscopy images showing E-Cadherin (red, white arrows) and nuclei (DAPI, blue). Scale bar: 20 μm. All data are shown as means ± SEM. Values shown are P values and were calculated using a two-tailed Student’s t-test (b, c, e, f, h) and one-way ANOVA with Tukey’s comparisons test (d, g) in GraphPad Prism 9.5.0. Source data are provided as a Source Data file.