Cat No:LP000034
CAS NO: 1217486-61-7
Molecular Formula: C19H22F3N5O2S
Molecular Weight: 441.47
Purity: 98% min
Solubility: In DMSO
Storage: -20°C
BYL-719 (NVP-BYL719) potently inhibits the 2 most common PIK3CA somatic mutations (H1047R, E545K; IC50~4 nM). BYL-719 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]. BYL-719 (BYL719) decreases cell proliferation by blocking cell cycle in G0/G1 phase with no outstanding effects on apoptosis cell death in HOS and MOS-J tumor cells. BYL-719 inhibits cell migration and can thus be considered as a cytostatic drug for osteosarcoma. In murine preclinical models of osteosarcoma, BYL-719 significantly decreases tumor progression and tumor ectopic bone formation as shown by a decrease of Ki67+ cells and tumor vascularization. BYL-719 rapidly inhibits the levels of P-AKT and P-mTOR in all cell lines assessed, confirming the functional activity of BYL-719 on osteosarcoma cells. After 72 hr of treatment, BYL-719 significantly inhibits the cell growth of all osteosarcoma cell lines tested in a dose-dependent manner with an IC50 ranging from 6 to 15 µM and with the IC90 from 24 to 42 µM at 72 hr[3].
