SNS-314 Mesylate
作者：齐岳
发布时间：2023-09-13
16:51:46
点击数：
产品名称：SNS-314 Mesylate
产品描述：
| 产品描述 | SNS-314 Mesylate 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 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 52.7 mg/mL (100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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