Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SNS-314 Mesylate (SNS-314) 是一种有效且特异性的极光激酶抑制剂,对极光激酶 A、B、C 的 IC50值分别为 9,31 和 3 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 247 | 现货 | ||
2 mg | ¥ 352 | 现货 | ||
5 mg | ¥ 579 | 现货 | ||
10 mg | ¥ 892 | 现货 | ||
25 mg | ¥ 1,820 | 现货 | ||
50 mg | ¥ 2,650 | 现货 | ||
100 mg | ¥ 4,130 | 现货 | ||
500 mg | ¥ 8,750 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 668 | 现货 |
产品描述 | SNS-314 Mesylate (SNS-314) is an effective and specific Aurora A/B/C inhibitor (IC50: 9/31/3 nM). It is less inhibition of Trk A/B, Fms, Flt4, c-Raf, Axl, and DDR2. |
靶点活性 | Aurora A:9 nM, Aurora B:31 nM, Aurora C:3 nM |
体外活性 | 在HCT116 结肠移植瘤中,SNS-314的抗癌效果明显和持久.在人类乳腺癌,前列腺癌,肺癌(H1299和Calu-6),卵巢癌及恶性黑色素瘤的鼠移植瘤中,SNS-314(170 mg/kg)对肿瘤生长抑制率为54-91%. |
体内活性 | 用SNS-314和吉西他滨、卡铂、道诺霉素、氟尿嘧啶和SN-38连续处理使抗增殖效果加强,SNS-314和吉西他滨,多西他赛,或长春新碱联用有协同效果。SNS-314对肿瘤细胞系具有明显抑制作用(IC50:1.8-24 nM), 且不依赖于Aurora-A或Aurora-B的相对蛋白水平。 |
激酶实验 | Aurora-A Kinase Assay: Humanized mouse Aurora A (amino acids 107-403) is expressed in E. coli as described previously. For IC50 assays, compounds are titrated three-fold in DMSO and diluted 12.5-fold into assay buffer (10 mM Tris HCl pH 7.2, 10 mM MgCl2, 0.05% NaN3, 0.01% Tween-20, and 0.1% BSA). Compounds are then diluted 4-fold into assay buffer containing Aurora A and FAM-PKAtide at final concentrations of 2 nM and 50 nM, respectively. The kinase reaction is initiated by adding ATP in assay buffer at a final concentration of 10 mM and incubated at 21 °C for 25 minutes. As a positive control, DMSO is added instead of compound and as a negative control assay buffer is added instead of Aurora A. Both control reactions are conducted in triplicate. To detect phosphorylated PKAtide, the kinase reaction is combined with Progressive Binding Solution (1:400 Progressive Binding Reagent, 1 × Buffer A, Molecular Devices) in a 1:3 ratio. The mixture is incubated for 30 minutes at 21 °C and the plate is scanned on an Analyst AD with excitation at 485 nm and emission at 530 nm. The percent relative enzymatic activity is calculated by normalizing the mP value for each well to the average positive control. Relative enzymatic activity values are plotted as a function of the logarithm of compound concentration and IC50 values are generated in GraphPad Prism software using a sigmoidal dose-response curve-fit. IC50's are calculated as the concentration of compound at which enzymatic activity i |
细胞实验 | Viability is measured using the CellTiter-Blue cell viability assay. Cells are treated as described above, although with a 5-day incubation period. Cytotoxicity is determined by measuring intracellular ATP using the CellTiter-Glo Luminescence Cell Viability Assay. Cells are seeded in white 96-well tissue culture plates at a density of 1.5-2 × 103 cells/well, and a serial dilution of SNS-314 is dosed in combination with fixed concentrations of either docetaxel or vincristine for a total of 72 hours. Viability is determined as the ratio between the ATP in treated cells versus control cells. Apoptosis is measured using the caspase-Glo 3/7 system. Cells are plated in white 96-well plates as described above and treated first with SNS-314 for 24 hours, washed with 200 μL of 1× PBS, and fresh medium is added with the second agent for 24 hours.(Only for Reference) |
别名 | SNS-314 |
分子量 | 527.04 |
分子式 | C18H15ClN6OS2·CH4O3S |
CAS No. | 1146618-41-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 52.7 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8974 mL | 9.4869 mL | 18.9739 mL | 47.4347 mL |
5 mM | 0.3795 mL | 1.8974 mL | 3.7948 mL | 9.4869 mL | |
10 mM | 0.1897 mL | 0.9487 mL | 1.8974 mL | 4.7435 mL | |
20 mM | 0.0949 mL | 0.4743 mL | 0.9487 mL | 2.3717 mL | |
50 mM | 0.0379 mL | 0.1897 mL | 0.3795 mL | 0.9487 mL | |
100 mM | 0.019 mL | 0.0949 mL | 0.1897 mL | 0.4743 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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