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AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of IR (IC50=57 μM). Tyrphostin AG 1024 prevents the growth inhibition for IC20 plus irradiation (4 Gy) by 50% compared to the control.Examination of Tyrphostin AG 1024 effects on radiation response demonstrates a marked enhancement in radiosensitivity and amplification of radiation-induced apoptosis. Tyrphostin AG 1024-induced apoptosis is associated with a downregulation of expression of phospho-Akt1, increased expression of Bax, p53 and p21, and a decreased expression of bcl-2 expression, especially when combined with irradiation. Tyrphostin AG 1024 is an effective anti-proliferative agent for breast carcinoma cells MCF-7. IGF1-R inhibitor tyrphostin AG1024 (10 μm) restores H358 cells apoptosis when cultured in serum-free medium. Incubation with AG1024 markedly decreases the AR level detected in the serum-free culture medium. AG1024 reduces IGF1 release in the serum-free culture medium. AG1024 enhances the apoptosis-inducing effect of gefitinib. Tyrphostin AG1024 significantly inhibits signal transmission by Akt (PKB), ERK (1/2), Src and STAT.The cytotoxic effect of AG1024 is more than 100 times greater on nutrient-deprived PANC-1 cells (NDM) with an IC50 of 55 nM, relative to cells in nutrient-sufficient medium (DMEM) with an IC50 of 21 μM. In DMEM, 0.3 μM AG1024 does not induce any significant PANC-1 cell death as determined using propidium iodide and annexin V staining and flow cytometry. In contrast, 34% of the cells grown in NDM and treated with the same concentration of AG1024 reveals propidium iodide-positive/annexin V-negative staining. In addition, AG1024 gives rise to significant increases in neuronal ADDL binding both when AG1024 is added alone and in the presence of exogenous insulin.
 |
Source | Oncotarget (2016). Figure 3. AG-1024 |
| Method | IGF-1R signaling analyses | |
| Cell Lines | NSCLC U-1810 cells | |
| Concentrations | 10 μmol/L | |
| Incubation Time | 24 hours | |
| Results | Interestingly, when cells were exposed to AG1024, a kinase inhibitor of IGF-1R at an IC50- dose IGF-1R β signals still remained illustrating that this TKI is not completely depleting IGF-1R β from the cells |
| Cell Experiment | |
|---|---|
| Cell lines | MCF-7 |
| Preparation method | 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. |
| Concentrations | Dissolved in DMSO, final concentration 10 μM |
| Incubation time | 24, 48 or 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | Female nude mice implanted subcutaneously with Ba/F3-p210 cells |
| Formulation | Dissolved in DMSO, and diluted in PBS |
| Dosages | 30 μg/day |
| Administration | Injected i.p |
| Molecular Weight | 305.17 |
| Formula | C14H13BrN2O |
| CAS Number | 65678-07-1 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[4] Maria Laura Giuffrida, et al. Beta-amyloid monomers are neuroprotective
[5] B Wen, et al. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells
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