ETP-46321

ETP-46321, has been pro?led and shown to be a potent PI3K a and d inhibitor, highly selective versus mTOR and 288 representative kinases. The compound demonstrated a good pharmacokinetic profile in mice and was selected for preliminary in vivo evaluation in a lung tumor mouse model driven by a K-Ras G12V oncogenic mutation, showing significant tumor growth inhibition (ca. 51%), and reduction of the tumor metabolic activity as measured by PET techniques.