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SNS-314 Mesylate Aurora Kinase inhibitor

Cat.No.S8699

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 and less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2.
SNS-314 Mesylate Aurora Kinase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 527.04

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Chemical Information, Storage & Stability

Molecular Weight 527.04 Formula

C18H15ClN6OS2.CH4O3S

 Storage (From the date of receipt)
CAS No. 1146618-41-8 -- Storage of Stock Solutions

Synonyms N/A Smiles CS(=O)(=O)O.C1=CC(=CC(=C1)Cl)NC(=O)NC2=NC=C(S2)CCNC3=NC=NC4=C3SC=C4

Solubility

In vitro
Batch:

DMSO : 86 mg/mL (163.17 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
Aurora C [1]
(Cell-free assay)
3 nM
Aurora A [1]
(Cell-free assay)
9 nM
Aurora B [1]
(Cell-free assay)
31 nM
In vitro
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[2]. A recent study shows that this compound shows potent antiproliferative activity in HCT116 cells and inhibits soft agar colony formation[3].
In vivo
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 this compound as single agents produce no significant inhibition of HCT116 tumor growth[2]. In the HCT116 human colon cancer xenograft model, administration of 50 and 100 mg/kg of this agent results a dose-dependent inhibition of histone H3 phosphorylation, indicating effective Aurora-B inhibition in vivo. In addition, HCT116 tumors from animals treated with this chemical exhibits potent and sustained responses including reduction of phosphorylated histone H3 levels, increased caspase-3 and appearance of increased nuclear size[3].
References

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