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CAS No.: 1146618-41-8

SNS-314 mesylate Catalog No. CSN18798

Synonyms: SNS-314 (mesylate);SNS-314

SNS-314 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.

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技术信息

生物活性

描述The Aurora family of serine/threonine kinases (Aurora-A, Aurora-B, and Aurora-C) plays a key role in cells orderly progression through mitosis. SNS-314 is a novel, potent, and selective inhibitor of Aurora kinases A, B, and C^[3]. In the HCT116 human colon cancer xenograft model, administration of 50 and 100 mg/kg SNS-314 led to dose-dependent inhibition of histone H3 phosphorylation for at least 10 h, indicating effective Aurora-B inhibition in vivo. HCT116 tumors from animals treated with SNS-314 showed potent and sustained responses including reduction of phosphorylated histone H3 levels, increased caspase-3 and appearance of increased nuclear size. The compound showed significant tumor growth inhibition in a dose-dependent manner under a variety of dosing schedules including weekly, bi-weekly, and 5 days on/9 days off^[4]. Treatment of the different ATC cells with SNS-314 mesylate inhibited proliferation in a time- and dose-dependent manner, with IC(50) comprised between 2.6 nM and 26.6 nM. CAL-62 cells exposed for 24 h to SNS-314 mesylate 100 nM evidenced a significant augmentation of the apoptotic index. Time-lapse video-microscopy of CAL-62 cells showed that SNS-314 mesylate prevents the completion of mitosis leading to polyploidy. Western blot experiments demonstrated that the auto-phosphorylation of the Aurora kinases as well as histone H3 phosphorylation in CAL-62 treated cells was inhibited. Finally, the drug inhibited colony formation in soft agar of all cell lines^[5]. Combination of Quercetin and SNS-314 leads to a synergistic cytotoxic effect on medullary TT and papillary BCPAP cell lines with a significant reduction of the IC50 value^[6].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 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

技术信息

CAS号	1146618-41-8	储存条件	粉末 Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C19H19ClN6O4S3	运输	蓝冰
分子量	527.04	别名	SNS-314 (mesylate);SNS-314

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