PI3Kalpha-IN-29 is an efficacious, orally bioavailable, and selective PI3Kalpha inhibitor with an IC50 value of 2.5 nM. It demonstrates over 400-fold selectivity against PI3Kbeta/delta/gamma/mTOR. This compound selectively degrades the H1047R mutant p110alpha protein and inhibits PI3Kalpha kinase activity. PI3Kalpha-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.
Target:
Akt|||mTOR|||CDK|||PI3K|||Cadherin
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