CAY10506

CAY10506 (also known as PI3K Inhibitor VII) is a potent, small molecule inhibitor of phosphatidylinositol 3-kinase (PI3K), originally discovered by researchers at Astellas Pharma (formerly Yamanouchi). It acts as an ATP-competitive antagonist, targeting the PI3K/Akt/mTOR signaling pathway, which is a critical regulator of cell growth, proliferation, and survival. Dysregulation of this pathway is a hallmark of various human cancers, making PI3K a significant therapeutic target. CAY10506 has been widely utilized as a tool compound in large-scale pharmacogenomic screens, most notably within the Cancer Therapeutics Response Portal (CTRP) and the Cancer Cell Line Encyclopedia (CCLE), to characterize the sensitivity of diverse cancer cell lines to PI3K inhibition. By blocking the phosphorylation of phosphatidylinositol-4,5-bisphosphate (PIP2) into phosphatidylinositol-3,4,5-trisphosphate (PIP3), CAY10506 effectively inhibits the recruitment and activation of Akt, thereby inducing growth arrest and apoptosis in susceptible malignant cells.

Other names

4-[4-[[4-(4-methylpiperazin-1-yl)phenyl]amino]quinazolin-6-yl]phenol