Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SH5-07 是一种基于异羟肟酸的 Stat3 抑制剂,IC50值为 3.9 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 497 | 现货 | ||
2 mg | ¥ 729 | 现货 | ||
5 mg | ¥ 1,230 | 现货 | ||
10 mg | ¥ 1,980 | 现货 | ||
25 mg | ¥ 3,370 | 现货 | ||
50 mg | ¥ 4,890 | 现货 | ||
100 mg | ¥ 6,860 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,690 | 现货 |
产品描述 | SH5-07 is a hydroxamic acid-based Stat3 inhibitor (IC50: 3.9 μM). |
靶点活性 | STAT3:3.9 μM (cell free) |
体外活性 | SH5-07是BP-1-102的羟胺酸类似物。SH5-07剂量依赖性抑制Stat3活性(IC50: 3.9±0.6 μM,体外实验)。它优先抑制Stat3:Stat3 DNA结合活性,而不是Stat1:Stat3活性,并对Stat1:Stat1活性影响最小。SH5-07与Stat3结合,破坏Stat3与生长因子受体的关联,从而抑制Stat3磷酸化。SH5-07对携带持续活跃Stat3的恶性细胞产生抗肿瘤细胞效应。SH5-07能够抑制已知的Stat3调控基因的表达。经过24小时,5 μM SH5-07处理后,Bcl-xL、Bcl-2、c-Myc、Survivin、Cyclin D1和Mcl-1的表达减少。 |
体内活性 | 通过尾静脉注射或口服灌胃方式给予SH5-07能够抑制已建立的皮下小鼠异种移植的人类胶质瘤(U251MG)和乳腺(MDA-MB-231)肿瘤的生长,其大小范围为90-150 mm^3,这些肿瘤中存在异常活跃的Stat3,与之相关的是Mcl-1、c-Myc和Cyclin D1表达的降低。未观察到体重、血细胞计数或器官的总体解剖结构有显著变化,也没有明显的毒性迹象。 |
细胞实验 | Cells are treated with 0-8 μM agent for 24-48 h. For cell cycle profile analysis, cells are harvested and fixed with 70% ice-cold ethanol and stained with propidium iodide (PI). For apoptosis analysis, cells are collected and stained with FITC-Annexin V using the Apoptosis Detection Kit. Both the DNA content of cells and the Annexin V-positive cells are analyzed by the flow cytometer. Cell cycle phase distribution is analyzed using the Cell-Fit program. Data acquisition is gated to exclude cell doublets. |
动物实验 | Mice are injected subcutaneously in the left flank area with U251MG cells in 200 μL of PBS/Matrigel matrix, or MDA-MB-231 cells in 100 μL of PBS. Mice with tumors of 90-150 mm^3 (MDA-MB-231) or 150 mm^3 (U251MG) are grouped for identical mean tumor sizes, administered 3, 5 or 6 mg/kg SH5-07 via oral gavage daily or tail vein injection every 2 or 3 days, and monitored every 3-7 days. Tumor sizes are measured with calipers and converted to tumor volume. |
分子量 | 625.61 |
分子式 | C29H28F5N3O5S |
CAS No. | 1456632-41-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (79.92 mM), Sonification is recommended.
H2O: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.5984 mL | 7.9922 mL | 15.9844 mL | 39.961 mL |
5 mM | 0.3197 mL | 1.5984 mL | 3.1969 mL | 7.9922 mL | |
10 mM | 0.1598 mL | 0.7992 mL | 1.5984 mL | 3.9961 mL | |
20 mM | 0.0799 mL | 0.3996 mL | 0.7992 mL | 1.998 mL | |
50 mM | 0.032 mL | 0.1598 mL | 0.3197 mL | 0.7992 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。
SH5-07 1456632-41-9 JAK/STAT signaling Stem Cells STAT Inhibitor SH5 07 inhibit SH507 SH-5-07 inhibitor