Apitolisib (GDC-0980, RG-7422, GNE-390)

Description: Apitolisib (formerly also known as GDC0980, RG7422, GNE390) is a novel, potent, selective and orally bioavailable class I PI3K inhibitor with potential anticancer activity. It inhibits PI3Kalpha/beta/delta/gamma with IC50 of 5 nM/27 nM/7 nM/14 nM in cell-free assays, respectively. It is also a potent mTOR inhibitor with Ki of 17 nM in a cell-free assay, and highly selective versus other PIKK family kinases. Apitolisib is a dual PI3 kinase/mTOR inhibitor, is also a n orally available agent targeting phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinase in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. Apitolisib inhibits both PI3K kinase and mTOR kinase, which may result in tumor cell apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR.

References:Mol Cancer Ther. 2011 Dec; 10(12):2426-36.