[CAS NO. 1146618-41-8] SNS-314 Mesylate
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PRODUCTS SPECIFICATIONS [1146618-41-8]
Store
Catalog
SLK-S8699
Brand
Selleck
CAS
1146618-41-8
DESCRIPTION [1146618-41-8]
Overview
| MDL | MFCD16621142 |
|---|---|
| Molecular Weight | 527.04 |
| Molecular Formula | C18H15ClN6OS2.CH4O3S |
| SMILES | O=C(NC1=NC=C(CCNC2=C3C(C=CS3)=NC=N2)S1)NC4=CC=CC(Cl)=C4.CS(=O)(O)=O |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8974 mL | 9.4869 mL | 18.9739 mL |
| 5 mM | 0.3795 mL | 1.8974 mL | 3.7948 mL |
| 10 mM | 0.1897 mL | 0.9487 mL | 1.8974 mL |
| 50 mM | 0.0379 mL | 0.1897 mL | 0.3795 mL |
Description
SNS-314 Mesylate is a potent and selective inhibitor of , and 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.
Targets
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. A recent study shows that SNS-314 Mesylate shows potent antiproliferative activity in HCT116 cells and inhibits soft agar colony formation.
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 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.
References
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