名称 | AG1024 |
描述 | AG1024 (Tyrphostin) suppresses IGF-1R autophosphorylation(IC50=7 μM), and is less potent for IR(IC50=57 μM). |
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) |
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. |
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。 |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 57 mg/mL (186.8 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble)
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关键字 | IGF-1R | IGF1R | DNA-PKcs | phosphorylation | growth | AGS200 | Apoptosis | AG1024 | BCR-ABL | AGS-200 | Tyrphostin AG-1024 | AG-1024 | factor-1 | Insulin Receptor | anti-cancer | Inhibitor | Akt | inhibit | AG 1024 | Tyrphostin AG1024 |
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相关库 | 抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 已知活性化合物库 | 细胞因子抑制剂库 | 药物代谢杂质库 | 激酶抑制剂库 | 抗衰老化合物库 | 干细胞分化化合物库 | 酪氨酸激酶分子库 |