DESCRIPTION PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKB¦Á (IC50=0.5 nM) than PKA (IC50=450 nM).

PRICE 301

DESCRIPTION PF-AKT400 is an APT competitor inhibitor of AKR kinase. This compound was first described as compound 42 in J. Med. Chem. 2010, 53, 4615-4622 by a group of Pfizer scientists. The paper describes the design and synthesis of novel, ATP-competitive Akt inhibitors from an elaborated 3-aminopyrrolidine scaffold. Key findings include the discovery of an initial lead that was modestly selective and medicinal chemistry optimization of that lead to provide more selective analogues. Analysis of the data suggested that highly lipophilic analogues would likely suffer from poor overall properties. Central to the discussion is the concept of optimization of lipophilic efficiency and the ability to balance overall druglike propeties with the careful control of lipophilicity in the lead series. Discovery of the nonracemic amide series and subsequent modification produced an advanced analogue that performed well in advanced preclinical assays, including xenograft tumor growth inhibition studies, and this analogue was nominated for clinical development. The compound has no official name, has molecule weight 400.43. We temporally call this compound as PF-AKT400. (BOC Sciences Bioactive Compounds)

DESCRIPTION PF-AKT400 (AKT protein kinase inhibitor) is a broadly selective and ATP-competitive inhibitor of Akt. (TargetMol Bioactive Compound Library)