SNS-314 Mesylate 1146618-41-8

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Molecular Weight:

527.04 SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1.


Biological Activity


In HCT116 colorectal carcinoma cell line, with intact or depleted p53
protein levels, SNS-314 Mesylate shows enhanced efficacy when
administered sequentially with other standard chemotherapeutic agents
and the most profound synergies are identified for agents that activate
the spindle assembly checkpoint, e.g., docetaxel and vincristine. A recent study shows that SNS-314 Mesylate shows potent
antiproliferative activity in HCT116 cells and inhibits soft agar colony
formation.


The sequential treatment with SNS-314 Mesylate followed by docetaxel 24
hours later produces a significant 72.5% tumor growth inhibition of
HCT116 xenografts, while docetaxel and SNS-314 Mesylate as single agents
produce no significant inhibition of HCT116 tumor growth.


In the HCT116 human colon cancer xenograft model, administration of 50
and 100 mg/kg SNS-314 Mesylate results a dose-dependent inhibition of
histone H3 phosphorylation, indicating effective Aurora-B inhibition in
vivo. In addition, HCT116 tumors from animals treated with SNS-314
Mesylate exhibits potent and sustained responses including reduction of
phosphorylated histone H3 levels, increased caspase-3 and appearance of
increased nuclear size.

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Product Categories : Epigenetics > Aurora Kinase Inhibitor