SAR156497
Product Specifications
CAS Number
1256137-14-0
Target
Others, PDE, Aurora Kinase
Related Pathways
Metabolism, Cell Cycle/Checkpoint, Others, Chromatin/Epigenetic
Bioactivity
SAR156497 is an exquisitely selective Aurora A, B, and C inhibitor with in vitro and in vivo efficacy with IC50 = 0.5 nM (Aurora A) ; 1 nM (Aurora B / incenp) ; 3 nM (Aurora C / incenp) respectively SAR156497 combines high in vitro potency with satisfactory metabolic stability and limited CYP 3A4 and PDE3 inhibition. In vitro, SAR156497 displayed high antiproliferative activity on a large panel of tumor cell lines without correlation with any particular genetic signature or Aurora kinases expression. It induced significant modulation of Aurora A and Aurora B biomarkers (p-Aurora A and pHH3, respectively) and cell polyploidy, as expected from Aurora A/B inhibitors.
Smiles
O=C1C=2[C@H](C=3C(=C(C(OCC)=O)NC3)NC2CCC1)C4=CC(OC=5NC=6C(N5)=CC=CC6)=CC=C4
Molecular Formula
C27H24N4O4
Molecular Weight
468.5
Shipping Conditions
Ice Packs
Storage Temperature
-20°C
Available Sizes
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