GSK2126458 is a highly potent PI3K and mTOR inhibitor with an app Ki of 19 pM for PI3K. In vivo, GSK2126458 showed anti-tumor activity in both pharmacodynamic and tumor growth efficacy models. In cell, in good agreement with the inhibition of potent PI3K. GSK2126458 reduced the phosphorylated AKT, p70S6K contents in a dose and time dependent way, as well as the prevention of PRAS40 and ERK. The IC50 of GSK2126458 is 2 nM for pAKT in the HCC1954 breast carcinoma cell line. In various human tumor cells, GSK2126458 had a width of inhibitory activity for potent cell growth and induced cell death. Notably, GSK2126458 acted mainly by not induction of apoptosis but cell cycle arrest, particularly in G1-phase.

June 21, 2017

prudect name : GSK2126458 is a highly potent PI3K and mTOR inhibitor with an app Ki of 19 pM for PI3K. In vivo, GSK2126458 showed anti-tumor activity in both pharmacodynamic and tumor growth efficacy models. In cell, in good agreement with the inhibition of potent PI3K. GSK2126458 reduced the phosphorylated AKT, p70S6K contents in a dose and time dependent way, as well as the prevention of PRAS40 and ERK. The IC50 of GSK2126458 is 2 nM for pAKT in the HCC1954 breast carcinoma cell line. In various human tumor cells, GSK2126458 had a width of inhibitory activity for potent cell growth and induced cell death. Notably, GSK2126458 acted mainly by not induction of apoptosis but cell cycle arrest, particularly in G1-phase.
GSK 2126458

Synonyms: GSK-2126458CAS NO: 1086062-66-9Molecular Formula: C₂₅H₁₇F₂N₅O₃SMolecular Weight: 505.50Purity: 98% minSolubility: In DMSOStorage: −20°C

RO4917838 References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18515597