Effect of caboznatinib on transcriptome and signaling pathways in leukemic cell line K562

To identify molecular effects of the tyrosine kinase inhibitor cabozantinib (XL184), we applied gene expression profiling in human erythroid leukemic cell lines K562 using Whole Transcriptome Shotgun Sequencing (RNA-seq). After K562 cell were treated with 1uM cabozantinib for 48 h, differentially expressed genes (DEGs) of 241 genes upregulated and 569 were downregulated were found compared with vehicle group. Up-regulated genes enriched in erythroid maturation associated pathways, such as heme metabolism, transcription factor GATA1 targets, and globin synthesis, while those genes downregulated after expose to cabozantinib were enriched in pathways involved in cell proliferation and cell survival function. Overall design: Gene expression in K562 was measured after exposure for 48 h to 1uM cabozantinib (XL184) or to the vehicle control (DMSO).