pictilisib-gdc-0941

Description: Pictilisib (also called GDC-0941, Pictrelisib, RG-7321 and GNE-0941) is a potent and orally bioavailable inhibitor of PI3Kalpha/delta (class I phosphatidylinositol 3 kinase) with IC50 of 3 nM in cell-free assays. It has potential anticancer activity and showed modest selectivity against p110beta (11-fold) and p110gamma (25-fold). Activation of PI3K/Akt signaling pathway is frequently associated with tumorigenesis. Deregulation of this pathway occurs frequently with a variety of cancers and may contribute to the resistance to many anticancer agents. Developing novel small molecules that specifically block the PI3K/Akt pathway may inhibit tumor growth. GDC-0941 is designed to bind the ATP-binding pocket of PI3K and to prevent formation of phosphatidylinositol-3, 4, 5-triphosphate (PIP3), a second messenger that transmits PI3K downstream signals. It binds to PI3K in an ATP-competitive manner.

References: Oncogene. 2008 Sep 18; 27(41):5497-510; J Med Chem. 2008 Sep 25; 51(18):5522-32.