PHT-427 is an AKT inhibitor that inhibits AKT and PDPK1 at low micromolar concentrations in numerous cancer cell lines and exhibits good oral anti-tumor activity in mouse xenograft models. PHT-427 reduces the phosphorylation of AKT and PDPK1. Following the administration of a single oral dose of PHT-427 to mice bearing BxPC-3 human pancreatic tumor xenografts, PHT-427 inhibited the phosphorylation of both Akt and PDPK1 as well as downstream targets maximally at 8–12 h after administration corresponding to its peak plasma concentration, with PDPK1 inhibition extending to 24 hr.
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MK-2206 2HCl; Ipatasertib; Triciribine; Capivasertib; Perifosine; CCT128930; AT7867; AT13148; ONC-201; Akti-1/2; SC66; Miltefosine; GSK690693