WAY-600

WAY-600 is a selective single digit nanomolar ATP-competitive mTOR inhibitor with an IC50 of about 9 nM. It has significant selectivity for these enzymes over phosphatidylinositol 3-kinase (PI3K) isofoms (>100-fold). With the 11% suppression by rapamycin, WAY-600 treated HEK293 cells indicated a 50% inhibition of polysomes. And WAY-600 blocked mTORC2-dependent phosphorylation of AKT in vitro and in vivo acutely. Without significant inhibition of P-AKT(T308), WAY-600 inhibited the mTORC1 substrate P-S6K(T389) and mTORC2 substrate P-AKT(S473) at submicromolar concentrations in various cancer cells.