AG-1024

Catalog No.S1234 Synonyms: Tyrphostin, AGS 200

AG-1024  Chemical Structure

Molecular Weight(MW): 305.17

AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, is less potent to IR with IC50 of 57 μM and specifically distinguishes between InsR and IGF-1R (as compared to other tyrphostins).

Size Price Stock Quantity  
In DMSO USD 150 In stock
USD 120 In stock
USD 210 In stock

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2 Customer Reviews

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    (A) CLL B cells purified from freshly isolat ed or freeze-thawed PBMCs from CLL patient samples were treated with a single dose of 15 µM AG1024, 1µM PPP or 1µM linsitinib for 24h and cell survival was determined by flow cytometry. Results are shown as mean  ± SEM, n=20. (B)CLL B cells purified from freshly isolat ed or freeze-thawed PBMCs from CLL patient samples were treated with a single dose of 15 µM AG1024 (AG) or 1µM linsitinib (L) and immunoblotted for the expression of phosphorylated IGF1R and IRS-1 (n=6). (C) CLL B cells purified from freshly isolat ed or freeze-thawed PBMCs from CLL patient samples were treated with a single dose of 1µM PPP and immunoblotted for the expression of phosphorylated IGF1R and IRS-1 (n=4). (D) CLL B cells purified from freshly isolated or freeze-thawed PBMCs from CLL patient samples were treated with 5-15 µM AG1024 and subject to a Western blot analysis using the indicated antibodies. Results are represented as mean±SEM (n=10). Supplementary Figure 1C shows the associated densitometrical analysis after treatment with 15 µM AG1024. (E) CLL B cells purified from freshly isolat ed or freeze-thawed PBMCs from CLL patient samples were treated with 10-500nM rhIGF-1 and immunoblotted for the expression of IGF1R, pIGF1R, pAkt, Akt, pERK and Erk. A representative example from four independent experiments is shown.

    Blood 2013 122(9), 1621-33. AG-1024 purchased from Selleck.

    FIG. 7. Gossypol sensitizes cancer cells to growth factor signaling pathway inhibitors. A, Forty-eight-hour treatments with the MEK inhibitor AZD6244 significantly reduced lung cancer A549 cell viability in a dose-dependent manner (0.1, 2, 5, and 10 μM) when combined with1 or 2 μM gossypol. B, Seventy-two-hour treatments with the EGFR inhibitor AG1478 (0.25, 0.5, and 1 μM) combined with 0.25 μM gossypol reduced cell viability in SKBR3 breast cancer cells. C, A 48-h treatment with the IGF-IR inhibitor AG1024 (0.25 and 0.5 μM) combined with 1 μM gossypol reduced cell viability in MCF-7 breast cancer cells. Serum-starved cells were incubated with vehicle (DMSO) as a control or with gossypol combined with inhibitors at indicated doses for 48-72 h. Cell viability with the different treatments was determined by MTS assays. Collected data were normalized to the DMSO treatment control, which was set to 100%. Each data point represented the average of values obtained from three wells of cells for each treatment. Differences between the untreated control and the inhibitor-treated samples were analyzed for the significance of difference using a Student’s t test, with P values indicated.

    Mol Endocrinol 2011 25, 2041-53. AG-1024 purchased from Selleck.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, is less potent to IR with IC50 of 57 μM and specifically distinguishes between InsR and IGF-1R (as compared to other tyrphostins).
Targets
IGF-1R [1] Insulin Receptor [1]
7 μM 57 μM
In vitro

AG-1024 blocks the IGF-1 receptor and IR autophosphorylation with IC50 of 7 μM and 57 μM, respectively. AG-1024 also inhibits the receptor tyrosine kinase activity towards exogenous substrates (TKA) with IC50 values of 18 μM and 80 μM, respectively. [1] AG-1024 (10 μM) inhibits cell proliferation in a time-dependent manner, and induces apoptosis in MCF-7 cells at 48 hours by 20.1% and >40% when combined with irradiation (10 Gy), more potently than that of irradiation (10 Gy) alone by 11.8%, which is associated with a down-regulation of phospho-Akt1 and bcl-2, and up-regulation of Bax, p53 and p21. [2] AG-1024 significantly inhibits melanoma cell proliferation with an IC50 of <50 nM in the absence of serum, by blocking MAPK/ERK2 signaling, subsequently rapidly inducing pRb dephosphorylation and activation, and eventually the formation of growth suppressive pRb-E2F complexes. [3] AG-1024 treatment down-regulates the expression of Bcr-Abl and P-Akt, and up-regulates DNA-PKcs expression in UT7-9 and Ba/F3-p210 cells, leading to decreased clonogenic survival and proliferation. AG-1024 also significantly inhibits the proliferation of cells resistant to the BCR-ABL inhibitor STI571, which correlates with a dose-dependent decrease in Bcr-Abl protein expression. [4]

In vivo Administration of AG-1024 at a dose of 30 μg for 10 days significantly inhibits the tumor growth of Ba/F3-p210 xenograft in mice. [4]

Protocol

Kinase Assay
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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.
Cell Research
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  • Cell lines: MCF-7
  • Concentrations: Dissolved in DMSO, final concentration 10 μM
  • Incubation Time: 24, 48 or 72 hours
  • 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.
    (Only for Reference)
Animal Research
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  • 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
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 61 mg/mL (199.88 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 305.17
Formula

C14H13BrN2O

CAS No. 65678-07-1
Storage powder
in solvent
Synonyms Tyrphostin, AGS 200

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IGF-1R Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID