AT13148

Description	AT13148 is a novel oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity, which shows a distinct mechanism of action from other AKT inhibitors. AT13148 is currently being developed by Astex Pharmaceuticals. AT131148 was identified utilizing high-throughput X-ray crystallography and fragment-based lead discovery techniques. AT13148 caused substantial blockade of AKT, p70S6K, PKA, ROCK and SGK substrate phosphorylation and induction of apoptosis in both a concentration and time-dependent manner in cancer cells with clinically relevant genetic defects both in vitro and in vivo.
Pathways	Cell Cycle/DNA Damage GPCR/G Protein TGF beta/Smad Wnt/Stem Cell PI3K/Akt/mTOR MAPK Pathway
Targets	ROCK PKA RSK AKT

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