Home>>Signaling Pathways>> Cell Cycle/Checkpoint>> Aurora Kinase>>SNS-314 Mesylate

SNS-314 Mesylate Sale

(Synonyms: N-(3-氯苯基)-N'-[5-[2-(噻吩并3,2-D]嘧啶-4-基氨基)乙基]-2-噻唑基]脲甲磺酸盐(1:1)) 目录号 : GC13837

A pan-Aurora kinase inhibitor

SNS-314 Mesylate Chemical Structure

Cas No.:1146618-41-8

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,008.00
现货
5mg
¥599.00
现货
10mg
¥1,061.00
现货
50mg
¥3,339.00
现货
200mg
¥8,211.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Kinase experiment:

A homogeneous time-resolved fluorescence (HTRF)-based biochemical IC50 assay is used to test for the kinase activity of the three isoforms of Aurora (A, B, and C) in the presence of SNS-314. A biotin-conjugated histone H3 peptide is used as substrate. Aurora-A kinase (7.5 nM) is assayed in 10 mM Tris–HCl pH 7.2, 10 mM MgCl2, 0.1% BSA, 0.05% Tween 20, 1 mM DTT, 120 nM biotinylated peptide ARTKQTARKSTGGKAPRKQLA-GGK-biotin, 6 μM ATP (2×the Km for the enzyme) for 1 h at 25°C. The reaction is stopped with 200 mM EDTA. Aurora-B and Aurora-C are assayed at 5 nM enzyme concentration, 120 nM biotinylated peptide, and 300 lM ATP (29 the Km for the enzymes) for 1 h at 25°C[2].

Cell experiment:

HCT116 cells are treated with various concentrations of SNS-314 for 96 hours. cells are incubated with BrdU for 2 h at 37°C. Cell proliferation activity is evaluated by chemiluminescence detection of BrdU incorporated in DNA[2].

Animal experiment:

Mice: Tumor mice are treated with vehicle or SNS-314. Animals are weighed, monitored for signs or symptoms of toxic effects, and measured for tumor volumes twice weekly until an end point is met[2].

References:

[1]. Oslob JD, et al. Discovery of a potent and selective aurora kinase inhibitor. Bioorg Med Chem Lett. 2008 Sep 1;18(17):4880-4.
[2]. Arbitrario JP, et al. SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17.

产品描述

SNS-314 is an ATP-competitive and selective inhibitor of aurora kinases with IC50 values of 9 nM, 31 nM and 3 nM against Aurora A, Aurora B and Aurora C, respectively [1 and 2].
Aurora kinases are serine/threonine kinases that regulate mitosis of cells. They are found to be associated with the onset and propagation of cancer and over-expressed in various tumor cell lines such as melanoma, ovarian, colon, pancreatic and breast tumors. Therefore, aurora kinases are being evaluated as potential targets in cancer therapy .As a potent inhibitor of aurora kinase, SNS-314inhibited proliferation in a broad panel of tumor cell lines and showed potent anti-tumor activity in mice bearing HCT116 xenografts. Besides that, a mechanism of its action was found to be inhibiting the phosphorylation of histoneH3 at Ser10 [1 and 2].
In the FRET-based biochemical assay, SNS-314inhibited Aurora A, B and C with IC50 values of 9, 31 and 3 nM, respectively. When tested against a panel of 219 kinases, SNS-314 only inhibited 24 kinases of them by 65% or above. It suggested that SNS-314 was a selective inhibitor of aurora kinase. In cell-based assays, SNS-314 blocked the proliferation of cancer cells with IC50 value in the range from 1.8 nM (A2780) to 24 nM (HT29). In HCT-116 cells, SNS-314 treatment for 16 hours resulted in distinct cell-cycle defects [2].
In human tumor xenograft mouse models, administration of SNS-314 exerted significant anti-tumor activities against xenografts of PC-3, H1299, A2780, MDA-MB-231 and A375 cells. The TGI value achieved between 54% and 91% when the dose was 170 mg/kg. The administration also caused a profound and sustained inhibition of pHH3 which was a substrate of Aurora B [2].
References:
[1] Oslob J D, Romanowski M J, Allen D A, et al. Discovery of a potent and selective aurora kinase inhibitor. Bioorganic & medicinal chemistry letters, 2008, 18(17): 4880-4884.
[2] Arbitrario J P, Belmont B J, Evanchik M J, et al. SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer chemotherapy and pharmacology, 2010, 65(4): 707-717.

Chemical Properties

Cas No. 1146618-41-8 SDF
别名 N-(3-氯苯基)-N'-[5-[2-(噻吩并3,2-D]嘧啶-4-基氨基)乙基]-2-噻唑基]脲甲磺酸盐(1:1)
化学名 1-(3-chlorophenyl)-3-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-1,3-thiazol-2-yl]urea;methanesulfonic acid
Canonical SMILES CS(=O)(=O)O.C1=CC(=CC(=C1)Cl)NC(=O)NC2=NC=C(S2)CCNC3=NC=NC4=C3SC=C4
分子式 C18H15ClN6OS2.CH4O3S 分子量 527.04
溶解度 ≥ 26.35 mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
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
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置