Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer

  • Bioorg Med Chem Lett. 2011 Mar 1;21(5):1315-9. doi: 10.1016/j.bmcl.2011.01.071.
Qing Dong  1 ,  Douglas R Dougan ,  Xianchang Gong ,  Petro Halkowycz ,  Bohan Jin ,  Toufike Kanouni ,  Shawn M O'Connell ,  Nicholas Scorah ,  Lihong Shi ,  Michael B Wallace ,  Feng Zhou
Affiliations
  • 1. Takeda San Diego, San Diego, CA 92121, USA.
PMID: 21310613 DOI: 10.1016/j.bmcl.2011.01.071
Abstract

A novel 5-phenylamino-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione series of MEK inhibitors has been developed using structure-based drug design. Lead optimization of this series led to the discovery of TAK-733. This was advanced to Phase I clinical studies for Cancer treatment.

Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-13449
    TAK-733
    99.79%, MEK Inhibitor
    target: MEK
    Research Areas: Cancer