| Cat.No.: | BSM-0012 |
| Product Name: | SNS-314 Mesylate |
| CAS No.: | 1146618-41-8 |
| Description: | 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. |
| Molecular Weight: | 527.04 |
| Storage: | 2 years -20°C Powder; 2 weeks 4°C in DMSO; 6 months -80°C in DMSO. |
| Targets: | Aurora A, Aurora B, Aurora C |
| IC50: | 9 nM; 31 nM; 3.4 nM |
| Molecular Formula: | C18H15ClN6OS2.CH4O3S |
| Chemical Name: | M1-(3-chlorophenyl)-3-(5-(2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl)thiazol-2-yl)urea Mesylate |
| Solubility: | DMSO 105 mg/mL; Water 6 mg/mL; Ethanol <1 mg/mL |
| 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. |
| Warning: | For Research Use Only! Not For Use in Humans. |
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