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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
AG-1024 (also called Tyrphostin or Tyrphostin AG1024) is a potent and selective inhibitor of IGF-1R (insulin-like growth factor-1) with potential antitumor activity. It has an IC50 of 7 μM, which selectively inhibits IGF-1R autophosphorylation, and an IC50 of 57 μM, which is less potent against Insulin receptor-IR. In a mouse model using a Ba/F3-p210 xenograft, AG-1024 demonstrates a notable antitumor efficacy.
Targets |
IGF1R (IC50 = 7 μM); IR (IC50 = 57 μM)
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
On 96-well plates (2,000–5,000 cells/well), NIH-3T3 cells overexpressing insulin receptors or IGF-1 are cultured and kept overnight in full medium. The cells are subsequently switched to 1% FBS-containing DMEM for 120 hours along with different concentrations of AG-1024 and 10 nM insulin or IGF-1. Every 48 hours, the medium is changed. Each well receives 100 μL of MTT after the medium has been aspirated out at the designated intervals. After incubating the cells for four hours at 37 °C, 100 μL of isoamylic alcohol is added, and the cells are shaken for twenty minutes to lyse them. The plate is then read between 570 and 690 nm in the ELISA reader. At the 120-hour time point, the IC50 value is computed.
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Cell Assay |
AG-1024 is applied to cells for 24, 48, or 72 hours. Trypan blue dye exclusion is used to harvest and count cells in order to determine the proliferation. By dual staining MCF-7 with propidium iodide and fluoresceine anti-digoxigenin, apoptosis is assessed. In summary, fixed cells are stored in a dark environment after being briefly washed with PBS, suspended in TdT buffer containing TdT enzyme and Dig-dUTP for 60 minutes, and suspended in FITC blocking solution containing anti-Dig-Fluorescein for 30 minutes at room temperature. Following a 30-minute resuspension in a propidium iodide/RNase A solution and a buffer rinse, the cells are flow-cytometrically examined. To evaluate phospho-Akt1, Bax, p53, bcl-2, and p21, lysed cells are subjected to western blot analysis.
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Animal Protocol |
Female nude mice implanted subcutaneously with Ba/F3-p210 cells
30 μg/day Injected i.p |
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References |
Molecular Formula |
C14H13BRN2O
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Molecular Weight |
305.17
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Exact Mass |
304.02
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Elemental Analysis |
C, 55.10; H, 4.29; Br, 26.18; N, 9.18; O, 5.24
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CAS # |
65678-07-1
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Appearance |
Solid powder
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SMILES |
CC(C)(C)C1=C(C(=CC(=C1)C=C(C#N)C#N)Br)O
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InChi Key |
ABBADGFSRBWENF-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C14H13BrN2O/c1-14(2,3)11-5-9(4-10(7-16)8-17)6-12(15)13(11)18/h4-6,18H,1-3H3
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Chemical Name |
2-[(3-bromo-5-tert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile
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Synonyms |
Tyrphostin; AG-1024; AG 1024; AG1024; Tyrphostin AG1024; Tyrphostin AG-1024
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.2769 mL | 16.3843 mL | 32.7686 mL | |
5 mM | 0.6554 mL | 3.2769 mL | 6.5537 mL | |
10 mM | 0.3277 mL | 1.6384 mL | 3.2769 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Dephosphorylation of pocket proteins in response to AG1024. Cancer Res. 2003 Mar 15;63(6):1420-9. |
pRb turnover in melanoma cells and normal melanocytes. Cancer Res. 2003 Mar 15;63(6):1420-9. td> |
pRb turnover in melanoma cells and normal melanocytes. Cancer Res. 2003 Mar 15;63(6):1420-9. td> |