Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AG1024 (Tyrphostin) 是一种可逆的,竞争性和选择性的胰岛素样生长因子-1 受体抑制剂,IC50为 7 μM。它抑制胰岛素受体的磷酸化,IC50值为 57 μM。它诱导细胞凋亡并具有抗癌活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 218 | 现货 | ||
5 mg | ¥ 496 | 现货 | ||
10 mg | ¥ 745 | 现货 | ||
25 mg | ¥ 1,250 | 现货 | ||
50 mg | ¥ 1,860 | 现货 | ||
100 mg | ¥ 2,980 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 546 | 现货 |
产品描述 | AG1024 (Tyrphostin) suppresses IGF-1R autophosphorylation(IC50=7 μM), and is less potent for IR(IC50=57 μM). |
靶点活性 | IGF-1R:7 μM, Insulin Receptor:57 μM |
体外活性 | 在携带有Ba / F3-p210异种移植物小鼠中,AG-1024(30 μg)施用10天能够显著抑制肿瘤生长. |
体内活性 | AG-1024能够阻断IGF-1受体(IC50=7 μM)和IR(IC50=57 μM)自磷酸化。在MCF-7 细胞中,AG-1024 (10 μM) 能够能够下调磷酸化Akt1和bcl-2,上调Bax,p53和p21,从而抑制细胞增殖。 |
激酶实验 | Inhibition of IGF-1- and insulin-stimulated cellular proliferation: NIH-3T3 cells overexpressing IGF-1 or insulin receptors are plated on 96-well plates (2,000-5,000 cells/well) and maintained overnight in complete medium. Cells are then changed to DMEM containing 1% FBS in the presence of 10 nM IGF-1 or insulin and various concentrations of AG-1024 for 120 hours. Medium is replaced every 48 hours. At the indicated periods of time, the medium is aspirated from the wells and 100 μL MTT is added to each well. The cells are then incubated for 4 hours at 37 °C and lysed by addition of 100 μL isoamylic alcohol and shaking for 20 minutes. The plate is then read in the ELISA reader at 570 and 690 nm. The IC50 value is calculated at the 120-hour time point. |
细胞实验 | Cells are exposed to AG-1024 for 24, 48 or 72 hours. For the determination of proliferation, cells are harvested and counted with trypan blue dye exclusion. Apoptosis is evaluated by dual staining of MCF-7 with fluoresceine anti-digoxigenin and propidium iodide. Briefly, fixed cells are washed with PBS, suspended in TdT buffer with TdT enzyme and Dig-dUTP for 60 minutes, and suspended in FITC blocking solution with anti-Dig-Fluorescein for 30 minutes at room temperature and kept in a dark place. Cells are then rinsed in buffer and resuspended in propidium iodide/RNase A solution for 30 minutes then analyzed by flow cytometry. For the assessment of phospho-Akt1, Bax, p53, bcl-2 and p21, cells are lysed and analyzed by western blot.(Only for Reference) |
别名 | Tyrphostin AG 1024, Tyrphostin, AGS 200 |
分子量 | 305.17 |
分子式 | C14H13BrN2O |
CAS No. | 65678-07-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 57 mg/mL (186.8 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.2769 mL | 16.3843 mL | 32.7686 mL | 81.9216 mL |
5 mM | 0.6554 mL | 3.2769 mL | 6.5537 mL | 16.3843 mL | |
10 mM | 0.3277 mL | 1.6384 mL | 3.2769 mL | 8.1922 mL | |
20 mM | 0.1638 mL | 0.8192 mL | 1.6384 mL | 4.0961 mL | |
50 mM | 0.0655 mL | 0.3277 mL | 0.6554 mL | 1.6384 mL | |
100 mM | 0.0328 mL | 0.1638 mL | 0.3277 mL | 0.8192 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。
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