Potent and selective dual ATP-competitive PI 3-K/mTOR inhibitor (Ki
values are 1.6, 1.8, 1.9, 2.1 and 16 nM for human PI 3-K δ
, and mTOR, respectively). Displays no significant inhibitory activity at more than 80 protein kinases (concentration ≥ 10 μ
M) including hVps34, PI 3-K downstream kinases, and MAPK family members. Orally available. Induces robust cell cycle arrest at the G1
phase in U87MG cancer cells and antitumor activity in SKOV3 ovarian cancer xenograft models.
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PF-04691502, a potent and selective oral inhibitor of PI3K and mTOR kinases with antitumor activity.
Yuan et al.
Mol.Cancer Ther., 2011;10:2189