AG-1024Selective IGF-1R inhibitor CAS# 65678-07-1 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 65678-07-1 | SDF | Download SDF |
| PubChem ID | 2044 | Appearance | Powder |
| Formula | C14H13BrN2O | M.Wt | 305.17 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Tyrphostin AG 1024 | ||
| Solubility | DMSO : ≥ 50 mg/mL (163.84 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 2-[(3-bromo-5-tert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile | ||
| SMILES | CC(C)(C)C1=C(C(=CC(=C1)C=C(C#N)C#N)Br)O | ||
| Standard InChIKey | ABBADGFSRBWENF-UHFFFAOYSA-N | ||
| Standard InChI | 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 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | AG-1024 is a selective inhibitor of IGF-1R with IC50 value of 7 μM. | |||||
| Targets | IGF-1R | |||||
| IC50 | 7 μM | |||||
| Cell experiment: [1] | |
| Cell lines | MCF-7 |
| Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
| Reacting condition | 10 nM, 5 days for cell proliferation inhibition 10 nM, 48 hours for apoptosis induction |
| Applications | The Tyrphostin AG-1024 induced a marked decrease of cell proliferation in a time-dependent manner. It also potently induced cell apoptosis with a 20.1 % of apoptotic cells. |
| Animal experiment : [2] | |
| Animal models | Female nude mice implanted with Ba/F3-p210 cells |
| Dosage form | Intraperitoneal injection, 30 μg in100 μl, once per day for 10 days |
| Application | After injection with Ba/F3-p210 cells (Bcr-Abl expressing cells), nude mice were injected after 6 days with PBS 0.1 ml (control) or Tyrphostin AG1024 30 μg/100 μl (1 μl of 980 μM). The growth of the Ba/F3-p210 xenografts was significantly delayed when mice were treated with Tyrphostin AG1024. |
| Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| References: [1] Wen B, Deutsch E, Marangoni E, et al. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells. British journal of cancer, 2001, 85(12): 2017. [2] Deutsch E, Maggiorella L, Wen B, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation. British journal of cancer, 2004, 91(9): 1735-1741. | |
AG-1024 Dilution Calculator
AG-1024 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.2769 mL | 16.3843 mL | 32.7686 mL | 65.5372 mL | 81.9216 mL |
| 5 mM | 0.6554 mL | 3.2769 mL | 6.5537 mL | 13.1074 mL | 16.3843 mL |
| 10 mM | 0.3277 mL | 1.6384 mL | 3.2769 mL | 6.5537 mL | 8.1922 mL |
| 50 mM | 0.0655 mL | 0.3277 mL | 0.6554 mL | 1.3107 mL | 1.6384 mL |
| 100 mM | 0.0328 mL | 0.1638 mL | 0.3277 mL | 0.6554 mL | 0.8192 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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AG1024 is an inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR) that specifically inhibits autophosphorylation of IGF-1R and IR with IC50 values of 7μM and 57 μm, respectively [1].
AG1024 has shown to inhibit IGF-1- and insulin-stimulated cellular proliferation in NIH-3T3 mouse fibroblast cells with IC50 values of 0.4μM and 0.1μM, respectively. Additionally, AG1024 shows to block tyrosine kinase activity towards exogenous substrates (TKA) with IC50 values of 18μM and 80μM [1].
AG1024 has been reported to block receptor tyrosine kinase activity, resulting in abolishment of MAPK and Akt pathways and inhibition of cell growth. Moreover, studies showed that AG1024 concentration-dependently inhibited E2 stimulation in MCF-7:PF cells [2].
References:
[1] Párrizas M1, Gazit A, Levitzki A, Wertheimer E, LeRoith D. Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997 Apr;138(4):1427-33.
[2] Fan P1, Agboke FA1, McDaniel RE1, Sweeney EE1, Zou X1, Creswell K1, Jordan VC2.Inhibition of c-Src blocks oestrogen-induced apoptosis and restores oestrogen-stimulated growth in long-term oestrogen-deprived breast cancer cells. Eur J Cancer. 2014 Jan; 50(2):457-68.
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Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells.[Pubmed:11747348]
Br J Cancer. 2001 Dec 14;85(12):2017-21.
Insulin-like growth factor-1 (IGF-1) plays an important growth-promoting effect by activating the PI3K/Akt signalling pathway, inhibiting apoptotic pathways and mediating mitogenic actions. Tyrphostin AG 1024, one selective inhibitor of IGF-1R, was used to evaluate effects on proliferation, radiosensitivity, and radiation-induced cell apoptosis in a human breast cancer cell line MCF-7. Exposure to Tyrphostin AG 1024 inhibited proliferation and induced apoptosis in a time-dependent manner, and the degree of growth inhibition for IC20 plus irradiation (4 Gy) was up to 50% compared to the control. Examination of Tyrphostin AG 1024 effects on radiation response demonstrated a marked enhancement in radiosensitivity and amplification of radiation-induced apoptosis. Western blot analysis indicated that Tyrphostin AG 1024-induced apoptosis was 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. To our knowledge, this is the first report showing that an IGF-1 inhibitor was able to markedly increase the response of tumour cells to ionizing radiation. These results suggest that Tyrphostin AG 1024 could be used as a potential therapeutic agent in combination with irradiation.
