SAR156497 - CAS 1256137-14-0

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.

Others, PDE, Aurora Kinase

Metabolism, Cell Cycle/Checkpoint, Others, Chromatin/Epigenetic

1256123

C27H24N4O4

468.5

O=C1C=2[C@H](C=3C(=C(C(OCC)=O)NC3)NC2CCC1)C4=CC(OC=5NC=6C(N5)=CC=CC6)=CC=C4

-20°C

Ice Packs

Small Compound