PF 05212384

Biological Activity

Potent and selective dual inhibitor of PI 3-kinase/mTOR (IC₅₀ values are 0.4, 1.6 and 5.4 nM for PI 3-Kα, mTOR and PI 3-Kγ respectively). Exhibits selectivity over 234 other protein kinases (IC₅₀ >10 μM). Potently inhibits tumor cell growth in 37 different tumor cell lines (IC₅₀ < 100 nM). Also exhibits antitumor activity in MDA-361, HCT-116, H1975 and U87MG xenograft models.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.

Additional Information

Background References

1. Bis(morpholino-1,3,5-triazine) derivatives: potent adenosine 5'-triphosphate competitive phosphatidylinositol-3-kinase/mammalian target of rapamycin inhibitors: discovery of compound 26 (PKI-587), a highly efficacious dual inhibitor.
   Venkatesan et al.
   J.Med.Chem., 2010;53:2636
2. Antitumor efficacy of PKI-587, a highly potent dual PI3K/mTOR kinase inhibitor.
   Mallon et al.
   Clin.Cancer Res., 2011;17:3193

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