PKI-402 is a selective, reversible, ATP-competitive, equipotent inhibitor of class I phosphatidylinositol 3-kinases (PI3K), including PI3K-alpha mutants, and mammalian target of rapamycin (mTOR; IC(50) versus PI3K-alpha = 2 nmol/L). PKI-402 inhibited growth of human tumor cell lines derived from breast, brain (glioma), pancreas, and non-small cell lung cancer tissue and suppressed phosphorylation of PI3K and mTOR effector proteins (e.g., Akt at T308) at concentrations that matched those that inhibited cell growth.
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Voxtalisib; Pilaralisib; PI-3065; VS-5584; PIK-294; AZD6482; GSK1059615; AZD8186; CUDC-907; AZD8835; AMG319; Buparlisib hydrochloride; Umbralisib; PIK-III; VPS34-IN1; VPS34 inhibitor 1; Wortmannin