Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Topo I/COX-2-IN-1 (1H-30) 是有效的 Topo I/COX-2抑制剂。Topo I/COX-2-IN-1抑制 COX-2 和 Topo I 的 IC50分别是 0.24 μM 和 4.42 μM。Topo I/COX-2-IN-1 能够诱导细胞凋亡 (apoptosis),抑制癌细胞迁移,显示出抗癌活性
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,600 | 10-14周 | ||
50 mg | ¥ 13,800 | 10-14周 | ||
100 mg | ¥ 17,500 | 10-14周 |
产品描述 | Topo I/COX-2-IN-1 (1H-30) is a potent Topo I/COX-2 inhibitor with the IC50 of 0.24 μM and 4.42 μM for COX-2 and Topo I, respectively. Topo I/COX-2-IN-1 induces apoptosis and inhibits migration of cancer cells, shows anti-cancer activity. |
体外活性 | Topo I/COX-2-IN-1 (1H-30) (0-100 μM, 24 h) has anti-tumor cell proliferation activity and can induce apoptosis by increasing caspase-3 activity in a dose-dependent manner [1]. Topo I/COX-2-IN-1 (1H-30) (0.04-0.37 μM, 48 h) shows a significant decrease in cell migration at 0.37 μM and reduces the expression of MMP-9 (matrix metalloproteinases) in HGC-27 and RKO cells [1]. Topo I/COX-2-IN-1 (1H-30) (10 μM, 48 h) can inhibit the activation of NF-κB pathway in cancer cells [1]. Cell Proliferation Assay [1] Cell Line: Colon cancer cell lines HGC-27, RKO, HT-29, SGC-7901, and CT26.WT Concentration: 0-100 μM Incubation Time: Result: Inhibited the proliferation of CT26.WT, RKO, HT-29, HGC-27 and SGC-7901 cells with the IC 50 values of 3.04, 3.12, 16.93, 4.71 and 14.95 μM, respectively. Apoptosis Analysis [1] Cell Line: HGC-27, RKO cell lines Concentration: 1.1 μM, 3.3 μM, 10 μM Incubation Time: 24 hours Result: Increased caspase-3 positive cells to 55.94% and 69.46 % at 10 μM comparing to 1.08% and 9.39% in the untreated group in RKO and HGC-27 cells respectively. Cell Cycle Analysis [1] Cell Line: HGC-27, RKO cell lines Concentration: 1.1 μM, 3.3 μM, 10 μM Incubation Time: Result: Induced blocked in G2/M phase significantly. |
体内活性 | Topo I/COX-2-IN-1 (1H-30) (intraperitoneal injection, 100 mg/kg, twice a day, 14 days) may inhibit tumor growth by increasing the expression of caspase-3 and decreasing MMP-9 and COX-2 in tumor tissues to induce apoptosis in BALB/c mice model infected with CT26.WT colon cancer cells [1]. Animal Model: BALB/c mice model infected with CT26.WT colon cancer cells [1] Dosage: 100 mg/kg Administration: Intraperitoneal injection; twice a day; 14 days Result: Significant reduction in tumor size and tumor weight and no significant differences in body weight, organs. Animal Model: SD rats [1] Dosage: 100 mg/kg Administration: Intraperitoneal injection; once Result: b>The pharmacokinetic parameters of Topo I/COX-2-IN-1 (1H-30) Parameter Topo I/COX-2-IN-1 (1H-30) t 1/2 1.56 h T max 0.67 h C max 20.19 μg/mL AUC 0-t 18.20 mg/L h AUC 0 inf_obs 18.60 mg/L h |
分子量 | 400.83 |
分子式 | C21H18ClFN2O3 |
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。
Topo I/COX-2-IN-1 Inhibitor inhibitor inhibit