DHW-221

DHW-221 is a potent dual inhibitor of PI3K and mTOR, demonstrating low nanomolar potency across all four Class I PI3K isoforms (PI3Kα, IC50 = 0.50 nM; PI3Kβ, IC50 = 1.9 nM; PI3Kγ, IC50 = 1.8 nM; PI3Kδ, IC50 = 0.74 nM) and mTOR (IC50 = 3.9 nM). This compound exhibits significant antitumor activity by disrupting the PI3K/Akt/mTOR signaling pathway, promoting mitochondrial apoptosis and paraptosis via endoplasmic reticulum stress and MAPK signaling, while also hindering cell cycle progression, migration, invasion, and angiogenesis. DHW-221 serves as a valuable tool in research related to non-small cell lung cancer (NSCLC), colon cancer, and breast cancer.