PKI-179

PKI-179 is a potent, orally active compound that functions as a dual PI3K/mTOR inhibitor. It demonstrates IC50 values of 8 nM for PI3K-α, 24 nM for PI3K-β, 74 nM for PI3K-γ, 77 nM for PI3K-δ, and 0.42 nM for mTOR. Additionally, it is effective against E545K and H1047R mutations, with IC50s of 14 nM and 11 nM, respectively. In vivo studies have shown that PKI-179 possesses anti-tumor capabilities[1][2].

PKI-179 hydrochloride is a potent and orally available dual PI3K/mTOR inhibitor. Its IC₅₀ values against PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR are 8 nM, 24 nM, 74 nM, 77 nM and 0.42 nM respectively. It also exerts inhibitory activity against E545K and H1047R mutants with IC₅₀ values of 14 nM and 11 nM, and exhibits significant antitumor effects in in vivo models.