afuresertib-gsk2110183

Description: Afuresertib (also named as GSK2110183C) is a potent, orally bioavailable and ATP-competitive Akt inhibitor with potential anticancer activity. It inhibits Akt1, Akt2, and Akt3 with Kis of 0.08 nM, 2 nM, and 2.6 nM, respectively. As an inhibitor of the serine/threonine protein kinase Akt (protein kinase B), Afuresertib has potential antineoplastic activity. Akt inhibitor GSK2110183 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

References: Cancer Chemother Pharmacol. 2015 Jan; 75(1):183-9; Blood. 2014 Oct 2; 124(14):2162-3.

Related CAS: 1047645-82-8 (Afuresertib HCl / GSK2110183B); 1047634-63-8 (GSK2110183); 2070009-64-0 (Afuresertib-F; GSK-2110183-analog HCl)