PI3Kα-IN-29

PI3Kα-IN-29 is an efficacious, orally bioavailable, and selective PI3Kα inhibitor with an IC50 value of 2.5 nM. It demonstrates over 400-fold selectivity against PI3Kβ/δ/γ/mTOR. This compound selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses the PI3K/AKT/mTOR signaling pathway, induces G1 phase arrest, and inhibits cell migration. Additionally, it impedes tumor growth in T47 mouse models and is applicable for breast cancer research.