Research Paper Volume 12, Issue 19 pp 19147—19158

VS-5584 exerts anti-survival, anti-proliferative, and pro-apoptotic activity in the established and primary human RCC cells. A498 cells, the primary human RCC cells (“RCC1/RCC2”) or HK-2 renal epithelial cells were treated with VS-5584 (5 μM), cells were further cultured for indicated time; PI3K-mTORC1/2 activation (A, B, Western blotting), cell survival (C, MTT), proliferation (D, BrdU EILSA and E, nuclei EdU staining), migration (F, “Transwell” assay) and apoptosis (G, ssDNA ELISA and H, TUNEL staining) were tested. The 786-O xenograft tumor-bearing nude mice were administrated with vehicle control (“Vehicle”, saline), VS-5584 (20 mg/kg, oral administration, daily), the tumor volumes (I) and mice body weights (J) were recorded every five days for a total of 35 days; The estimated daily tumor growth was calculated (K); Data were presented as mean ± standard deviation (SD). *p< 0.05 vs. “C” group (C–H, n=5). *p< 0.05 vs. “Vehicle” (I, J, n=10). The in vitro experiments were repeated four times, and similar results were obtained. Bar = 100 μm (E, F, H).