Powder: -20°C for 3 years | In solvent: -80°C for 1 year
STAT3-IN-10 (A11) 是一种STAT3抑制剂,可直接结合 STAT3 SH2 结构域,抑制肿瘤细胞生长并且诱导肿瘤细胞凋亡 (IC 50 = 5.18 μM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 6-8周 | ||
50 mg | ¥ 13,800 | 6-8周 | ||
100 mg | ¥ 17,500 | 6-8周 |
产品描述 | STAT3-IN-10 (A11) is an inhibitor of STAT3 that directly binds to STAT3 SH2 domain, inhibits tumor cell growth and induces apoptosis in cancer cells (IC 50 = 5.18 μM) [1]. |
体外活性 | STAT3-IN-10 (A11) (48 h) shows IC 50 values of 0.67, 0.77, 1.24 μM against MDA-MB-231, MDA-MB-468, HepG2 cells, respectively [1]. STAT3-IN-10 (A11) directly binds to the STAT3 SH2 domain [1]. STAT3-IN-10 (A11) (0-3 μM, 24 h) inhibits the phosphorylation of STAT3 and its downstream target proteins and has a good selectivity against the tumor suppressor STAT1 [1]. STAT3-IN-10 (A11) (0-4 μM, 24 h) induces apoptosis in cancer cells [1]. STAT3-IN-10 (A11) (0-4 μM, 24 h) dose-dependently causes a significant S phase arrest in MDA-MB-231 cells [1]. Cell Viability Assay [1] Cell Line: Breast cancer cell lines: MDA-MB-231 and MDA-MB-468; human liver carcinoma cell line: HepG2. Concentration: Incubation Time: 48 h, re-incubated for 4 h (MDA-MB-468, MDA-MB-231) and 1h (HepG2). Result: Showed IC 50 values of 0.67, 0.77, 1.24 μM against MDA-MB-231, MDA-MB-468, HepG2 cells, respectively. Western Blot Analysis [1] Cell Line: MDA-MB-231. Concentration: 0, 0.75, 1.5 and 3.0 μM. Incubation Time: 24 h. Result: Decreased the STAT3-Y705 phosphorylation without affecting the total amount of STAT3 protein and decreased the expression of STAT3 target genes, including C-Myc and Cyclin D1 in a dose-dependent manner. Had little impact on the level of STAT1 and its phosphorylation on Tyr701. Apoptosis Analysis [1] Cell Line: MDA-MB-231. Concentration: 0, 1, 2, and 4 μM. Incubation Time: 24 h. Result: Induced the apoptosis in MDA-MB-231 cells in a concentration-dependent manner Cell Cycle Analysis [1] Cell Line: MDA-MB-231. Concentration: 0, 1, 2, and 4 μM. Incubation Time: 24 h. Result: Could dose-dependently cause a significant S phase arrest in MDA-MB-231 cells |
体内活性 | STAT3-IN-10 (A11) (5 and 10 mg/kg; IP; once a day, 21 days) inhibits the growth of human xenograft tumor in vivo [1]. Animal Model: Five weeks old female BALB/c nude mice (16–18g) bearing inoculation of human breast cancer cells MDA-MB-231 [1]. Dosage: 5 and 10 mg/kg Administration: IP, once a day, 21 days Result: Inhibited the growth of human xenograft tumor in vivo without apparent body-weight loss for treated mice and inhibited the levels of p-STAT3 in tumor tissues. |
分子量 | 311.29 |
分子式 | C17H13NO5 |
CAS No. | 2499491-04-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
STAT3-IN-10 2499491-04-0 Inhibitor inhibitor inhibit