Catalog No.: PC-27801Not For Human Use, Lab Use Only.
Uprosertib (GSK2141795) is a potent, selective, ATP-competitive and orally bioavailable AKT inhibitor with IC50 of 0.066 nM, 1.4 nM and 1.5 nM for Akt1, Akt2 and Akt3 respectively.
Uprosertib (GSK2141795) is a potent, selective, ATP-competitive and orally bioavailable AKT inhibitor with IC50 of 0.066 nM, 1.4 nM and 1.5 nM for Akt1, Akt2 and Akt3 respectively.
Uprosertib (GSK2141795) inhibits the kinase activity of the E17K AKT 1 mutant protein with EC50 of 0.2 nM.
Uprosertib (GSK2141795) showes concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3β, PRAS40, FOXO and Caspase 9 in both cell lines, exhibits growth inhibition in human cancer cell lines.
Uprosertib (GSK2141795) (10, 20 and 30 mg/kg, QD) shows tumor growth inhibition (TGI) of 73, 85 or 93% in mice bearing BT474 tumors.
Combining Uprosertib (GSK2141795) with the AKT inhibitor or MEK inhibitor (GSK2110212; trametinib) resulted in an enhanced anti-tumor effect accompanied with greater reduction in phospho-S6 levels.
