XL418

XL418 is a selective, orally active small molecule dual inhibitor of protein kinase B (PKB or AKT) and ribosomal protein S6 kinase beta-1 (p70S6K or RPS6KB1), both of which are key components downstream of the phosphoinosotide-3 kinase (PI3K) signaling pathway. By inhibiting AKT and p70S6K, XL418 disrupts a pathway frequently activated in human tumors that promotes cell growth, survival, and resistance to chemotherapy and radiotherapy. Inactivation of this pathway through AKT inhibition is expected to induce apoptosis in tumor cells and may sensitize them to other anticancer therapies. Developed as an investigational anticancer agent by Exelixis, it entered phase I clinical trials for solid tumors but development was discontinued due to low drug exposure[1][2][3][4][5][7].

Other names

serine/threonine kinase inhibitor XL418