Figure 1.

Ponatinib reverses the expression of certain BCLM-associated genes. (A) The scheme of the experimental process. (B) Potential anti-metastatic compounds are sorted by the activity score of reversing the BCLM-associated gene signature. The top 5 hit compounds are shown as red dots. (C) Heat map representing the expression of 13 metastatic-related genes (up-regulated, red; down-regulated, blue) in MDA-MB-231 cells treated with the top 5 hit compounds in the screen data, the log₂ (fold change) is used to scale the differences in gene expression. (D) The top 5 chemical structures are shown. (E) LM2 cells or mouse breast cancer 4T1 cells were treated with 1 µmol/L Ponatinib at 24 h, heat map representing the expression of 6 metastatic-related genes in three independent experiments. (F and G) RT-qPCR analysis showed that Ponatinib was capable of reversing the expression of 6 BCLM-associated genes in a dose- and time-dependent manner. Cells were treated with a serial dilution of Ponatinib at 24 h (F) or with 1 µmol/L Ponatinib at various time points (0, 2, 4, 6, 12 and 24 h) (G). Data present mean ± SD of three independent experiments and normalized to DMSO control