Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GL0388 是一种Bax 激活剂,可导致 Bax 插入线粒体膜,从而诱导 Bax 介导的细胞凋亡。GL0388 在体内抑制乳腺癌异种移植的肿瘤生长,并且对多种癌细胞表现出抗增殖活性,IC50值为 0.299-1.57 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 8,900 | 10-14周 | ||
50 mg | ¥ 11,800 | 10-14周 | ||
100 mg | ¥ 17,500 | 10-14周 |
产品描述 | GL0388 is a Bax activator and leads to Bax insertion into mitochondrial membrane that induce Bax-mediated apoptosis. GL0388 inhibits tumor growth of breast cancer xenograft in vivo which also exhibits antiproliferative activities against a variety of cancer cells with IC50 values of 0.299-1.57 μM [1]. |
体外活性 | GL0388 (0.1-10 μM; 72 h) inhibits the cell proliferation of MDA-MB-231 and MCF-7 breast cancer cell lines, with IC 50 s of 0.96 μM and 0.52 μM, respectively [1]. GL0388 (0.01-100 μM) inhibits the cell proliferation in 60 human tumor cell lines, with GI5 50 s of 0.299-1.57 μM [1]. GL0388 (1-10 μM; 48 h) significantly upregulates the cleaved PARP-1 and cleaved caspase 3 in MDA-MB-231 cells [1]. GL0388 (0.1-1 μM; 24 h) inhibits the colony formation and invasion of breast cancer cells [1]. GL0388 (1-10 μM; 24 h) promotes Bax insertion into mitochondrial membranes of MDA-MB-231 cells in a dose-dependent manner. GL0388 increases cytochrome c in the cytosolic fraction of MDA-MB-231 cells [1]. Cell Proliferation Assay [1] Cell Line: MCF-7, MDA-MB-231 cells Concentration: 0.1, 0.33, 1, 3.3, 10 μM Incubation Time: 72 hours Result: Inhibited the growth of MCF-7, MDA-MB-231 cells, with IC 50 s of 0.52 μM and 0.96 μM, respectively. Western Blot Analysis [1] Cell Line: MDA-MB-231 cells Concentration: 1, 5, 10 μM Incubation Time: 48 hours Result: Significantly led to the upregulation of cleaved PARP-1 and cleaved caspase 3. |
体内活性 | GL0388 (10-20 mg/kg for i.p.; 15 mg/kg for i.t.; once daily for 10 days) dose-dependently suppresses the growth of MDA-MB-231 tumors in mice [1]. Animal Model: Female nude mice were injected MDA-MB-231 cells [1] Dosage: 10-20 mg/kg for i.p.; 15 mg/kg for i.t. Administration: I.p and i.t. once daily for 10 days Result: Significantly inhibited tumor growth at a dose of 15 mg/kg every other day. I.T. administration for 10 consecutive days, with an inhibition rate of 55%, comparable to the I.P. efficacy at the dose of daily 20 mg/kg. |
分子量 | 332.37 |
分子式 | C21H17FN2O |
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。
GL0388 Inhibitor inhibitor inhibit