| Name | AG1024 |
| Description | AG1024 (Tyrphostin) suppresses IGF-1R autophosphorylation(IC50=7 μM), and is less potent for IR(IC50=57 μM). |
| Cell Research | 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) |
| Kinase Assay | 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. |
| In vitro | In mice carrying Ba/F3-p210 xenografts, the administration of AG-1024 (30 μg) for 10 days significantly inhibited tumor growth. |
| In vivo | AG-1024 effectively inhibits autophosphorylation of the IGF-1 receptor (IC50=7 μM) and IR (IC50=57 μM). In MCF-7 cells, at a concentration of 10 μM, AG-1024 downregulates phosphorylated Akt1 and bcl-2, while upregulating Bax, p53, and p21, thereby inhibiting cell proliferation. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 75 mg/mL (245.76 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.55 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | Tyrphostin AG-1024 | Tyrphostin AG1024 | Insulin Receptor | IGF-1R | IGF1R | factor-1 | DNA-PKcs | BCR-ABL | Apoptosis | anti-cancer | AGS-200 | AGS200 | AG-1024 | AG1024 | AG 1024 |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Glycometabolism Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Kinase Inhibitor Library | Anti-Viral Compound Library | Inhibitor Library | Endocrinology-Hormone Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Cancer Active Compound Library |
United States
