AG-1024 (Synonyms: AGS 200, Tyrphostin AG1024) |
| Katalog-Nr.GC13697 |
AG-1024 (Tyrphostin AG 1024) ist ein reversibler, kompetitiver und selektiver IGF-1R-Inhibitor mit einem IC50 von 7 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 65678-07-1
Sample solution is provided at 25 µL, 10mM.
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AG-1024 is a reversible, competitive and selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 value of 7µM[1]. AG-1024 can inhibit the phosphorylation of insulin receptor (IR) with an IC50 value of 57µM[2]. AG-1024 can induce cell apoptosis and has anti-cancer activity[3].
In vitro, AG-1024 (5µM) treatment of acquired sorafenib-resistant cell lines (SNU-sora-5 and SK-sora-5 cells) for 72h significantly increased the cytotoxicity of sorafenib, activated the intracellular mTOR/P21 signaling pathway, and enhanced the cell G1/S arrest[4]. AG-1024 (10μM) treatment of PC3 and DU145 cells inhibited cell proliferation and induced cell G2/M phase arrest[5].
In vivo, oral administration of AG-1024 (20mg/kg) to diabetic nephropathy model rats for 8 weeks alleviated metabolic disorders, improved renal function, reduced renal inflammation, and reduced renal fibrosis formation[6].
References:
[1] Xue M, Cao X, Zhong Y, et al. Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors in cancer therapy: advances and perspectives[J]. Current pharmaceutical design, 2012, 18(20): 2901-2913.
[2] Talior-Volodarsky I, Mahou R, Zhang D, et al. The role of insulin growth factor-1 on the vascular regenerative effect of MAA coated disks and macrophage-endothelial cell crosstalk[J]. Biomaterials, 2017, 144: 199-210.
[3] Cheng H Y, Ko F H. Studying the enhancement of programmed cell death by combined AG1024 and paclitaxel in a model of chronic myelogenous leukemia[J]. Life sciences, 2014, 102(2): 118-126.
[4] Zhou W, Lou W, Chen J, et al. AG-1024 Sensitizes Sorafenib-Resistant Hepatocellular Carcinoma Cells to Sorafenib via Enhancing G1/S Arrest[J]. OncoTargets and therapy, 2021: 1049-1059.
[5] Tang Q, Ma J, Sun J, et al. Genistein and AG1024 synergistically increase the radiosensitivity of prostate cancer cells[J]. Oncology Reports, 2018, 40(2): 579-588.
[6] Liu J, Zhang Y, Liu M, et al. AG1024, an IGF-1 receptor inhibitor, ameliorates renal injury in rats with diabetic nephropathy via the SOCS/JAK2/STAT pathway[J]. Open Medicine, 2023, 18(1): 20230683.
| Cell experiment [1]: | |
Cell lines | SNU-sora-5、SK-sora-5 cells |
Preparation Method | SNU-sora-5 and SK-sora-5 were exposed to a series of concentrations of sorafenib with or without 5μM AG-1024 for 72h. The IC50 values of Sorafenib were determined. |
Reaction Conditions | 5µM; 72h |
Applications | AG-1024 dramatically improve the cytotoxicity of sorafenib in acquired sorafenib-resistant cells. |
| Animal experiment [2]: | |
Animal models | Wistar rats |
Preparation Method | Rats were randomly assigned into the control, the DN, the DN+AG-1024, and the DN+metformin groups. Each group had 15 rats. The overnight-fasted rats were intraperitoneally injected with 2% pentobarbital sodium (40mg/kg) followed by the removal of the right kidneys. The controls were injected once with citrate buffer and 0.5mL saline daily for 12 weeks. After 2 weeks, the rats in the DN groups received a single intraperitoneal injection of freshly prepared streptozotocin (STZ; 50mg/kg). After 4 weeks of cultivation, the diabetic rats in the DN group received 0.5mL saline daily, those in the DN+AG-1024 group were administered with AG-1024 (20mg/kg/day, p.o.), and those in the DN+metformin group were given with metformin (200mg/kg/day) by gavage for 8 weeks. |
Dosage form | 20mg/kg for 8 weeks; p.o. |
Applications | AG-1024 can reduce metabolic disorders in the experimental rat model of diabetic nephropathy. AG-1024 can improve renal function, reduce renal inflammation, and reduce renal fibrosis formation in diabetic rats. |
References: | |
| Cas No. | 65678-07-1 | SDF | |
| Überlieferungen | AGS 200, Tyrphostin AG1024 | ||
| Chemical Name | 2-[(3-bromo-5-tert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile | ||
| Canonical SMILES | CC(C)(C)C1=C(C(=CC(=C1)C=C(C#N)C#N)Br)O | ||
| Formula | C14H13BrN2O | M.Wt | 305.17 |
| Löslichkeit | ≥ 15.25mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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