| Identification | Back Directory | [Name]
SAR156497 | [CAS]
1256137-14-0 | [Synonyms]
SAR156497
SAR-156497; SAR 156497
YXMQIWJYPNBZJS-QFIPXVFZSA-N | [Molecular Formula]
C27H24N4O4 | [MDL Number]
MFCD28411357 | [MOL File]
1256137-14-0.mol | [Molecular Weight]
468.5 |
| Hazard Information | Back Directory | [Description]
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. | [Uses]
SAR156497 (compound 47) is an Aurora inhibitor, with IC50 values ??of 0.6 nM and 1 nM for Aurora A and Aurora B, respectively. SAR156497 can also inhibit PDE3, with IC50 value of 4 μM. SAR156497 can be used in anticancer research[1]. | [IC 50]
PDE3: 4 μM (IC50); Aurora A: 0.6 nM (IC50); Aurora B: 1 nM (IC50) | [References]
[1] Carry JC, et al. SAR156497, an exquisitely selective inhibitor of aurora kinases. J Med Chem. 2015 Jan 8;58(1):362-75. DOI:10.1021/jm501326k |
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| Company Name: |
BOC Sciences
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| Tel: |
16314854226 |
| Website: |
www.bocsci.com |
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