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Cat. No. M3397
AG-1024 Structure

Tyrphostin AG 1024

Size Price Availability Quantity
5mg USD 70 In stock
10mg USD 125 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

AG-1024 is a selective IGF-1R inhibitor with an IC50 of 0.4 μM. Exposure to Tyrphostin AG 1024 inhibits proliferation of cell and triggers their apoptosis in a time-dependent manner. 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.

Customer Product Validations & Biological Datas
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 305.17
Formula C14H13BrN2O
CAS Number 65678-07-1
Purity >98%
Solubility DMSO 55 mg/mL
Storage at -20°C
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Abmole Inhibitor Catalog 2017

Keywords: AG-1024, Tyrphostin AG 1024 supplier, IGF-1R, inhibitors

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