2. Academic Validation
  3. Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor

Identification of GNE-477, a potent and efficacious dual PI3K/mTOR inhibitor

  • Bioorg Med Chem Lett. 2010 Apr 15;20(8):2408-11. doi: 10.1016/j.bmcl.2010.03.046.
Timothy P Heffron 1,  Megan Berry,  Georgette Castanedo,  Christine Chang,  Irina Chuckowree,  Jennafer Dotson,  Adrian Folkes,  Janet Gunzner,  John D Lesnick,  Cristina Lewis,  Simon Mathieu,  Jim Nonomiya,  Alan Olivero,  Jodie Pang,  David Peterson,  Laurent Salphati,  Deepak Sampath,  Steve Sideris,  Daniel P Sutherlin,  Vickie Tsui,  Nan Chi Wan,  Shumei Wang,  Susan Wong,  Bing-Yan Zhu
Affiliations

Affiliation

  • 1 Discovery Chemistry, Genentech, Inc., South San Francisco, CA 94080, USA. [email protected]
PMID: 20346656 DOI: 10.1016/j.bmcl.2010.03.046
Abstract

Efforts to identify potent small molecule inhibitors of PI3 kinase and mTOR led to the discovery of the exceptionally potent 6-aryl morpholino thienopyrimidine 6. In an effort to reduce the melting point in analogs of 6, the thienopyrimidine was modified by the addition of a methyl group to disrupt planarity. This modification resulted in a general improvement in in vivo clearance. This discovery led to the identification of GNE-477 (8), a potent and efficacious dual PI3K/mTOR Inhibitor.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-11042
    98.70%, PI3K Inhibitor