Chemical Name: 2-Amino-8-[trans-4-(2-hydroxyethoxy)cyclohexyl]-6-(6-methoxy-3-pyridinyl)-4-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
Biological ActivityPotent 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, α, γ, β, and mTOR, respectively). Displays no significant inhibitory activity at more than 80 protein kinases (concentration ≥ 10 μM) 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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
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