In Vitro |
Alpelisib (BYL-719) potently inhibits the 2 most common PIK3CA somatic mutations (H1047R, E545K; IC50s~4 nM). Alpelisib potently inhibits Akt phosphorylation in cells transformed with PI3Kα (IC50=74±15 nM) and shows significant reduced inhibitory activity in PI3Kβ or PI3Kδ isoforms transformed cells (≥15-fold compared with PI3Kα)[2]. Alpelisib (BYL-719, 0-50 μM; 72 hours) inhibits the cell growth of osteosarcoma cell lines MG63, HOS, POS-1 and MOS-J in a dose-dependent manner[3]. Alpelisib (BYL-719) significantly alters the distribution of cell cycle phases. Alpelisib (BYL-719, 25 μM; 18 hours) induces a cell cycle arrest in the G0/G1 phase of human and murine osteosarcoma cell lines[3]. Cell Proliferation Assay[3] Cell Line: MG63, HOS, POS-1, MOS-J Concentration: 10, 20, 30, 40, 50 μM Incubation Time: 72 hours Result: Inhibited the cell growth of all osteosarcoma cell lines tested in a dose-dependent manner with IC50s of 6-15 µM and with IC90s of 24-42 µM. Cell Cycle Analysis[3] Cell Line: MG63, HOS, POS-1, MOS-J Concentration: 25 μM Incubation Time: 18 hours Result: Induced a cell cycle arrest in the G0/G1 phase of human and murine osteosarcoma cell.
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