AEterna Zentaris has identified a new generation of low molecular weight pyridopyrazine compounds as highly potent and selective inhibitors of class I PI3Ks. Presented here, are the key in vitro characteristics of AEZS-126 that led to its selection for in vivo development. AEZS-126 inhibits PI3Ka with an IC50 value of 10nM and proved to be a potent inhibitor of Akt phosphorylation in cellular assays. Mode-of-action studies showed that AEZS-126 acts as an ATP competitive compound. The in vitro antiproliferative activity against different human tumor cell lines (MDA-MB 468, U87, Hct116, PC-3, A549 and others) was determined, with EC50 values in the nanomolar range.
The optimization of AEterna Zentaris' pyridopyrazine lead structure regarding kinase selectivity, cellular potency and ADMET properties, led to the identification of AEZS-126, a compound which has a favorable in vitro pharmacologic profile for further in vivo profiling.
About AEterna Zentaris Inc.
AEterna Zentaris Inc. is a global biopharmaceutical company focused on endocrine therapy and oncology, with proven expertise in drug discovery, development and commercialization. News releases and additional information are available at www.aezsinc.com.
This press release contains forward-looking statements made pursuant to the safe harbor provisions of the U.S. Securities Litigation Reform Act of 1995. Forward-looking statements involve known and unknown risks and uncertainties, which c
|SOURCE AETERNA ZENTARIS INC.|
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