AG1024
Based on 6 publication(s) in Google Scholar
AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of IR (IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity.
For research use only. We do not sell to patients.
- Purity: 99.50%
- CAS No.: 65678-07-1
- Formula: C14H13BrN2O
- Molecular Weight:305.17
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) AG1024
More- Cell Commun Signal. 2024 May 27;22(1):292. [Abstract]
- Br J Pharmacol. 2021 Nov;178(21):4389-4407. [Abstract]
- J Invest Dermatol. 2023 May;143(5):832-841.e4. [Abstract]
- J Biol Chem. 2022 Mar;298(3):101645. [Abstract]
- Pflugers Arch. 2024 Dec;476(12):1913-1928. [Abstract]
- Biomed Pharmacother. 2017 Nov:95:1346-1358. [Abstract]
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IF
Biological Activity
AG1024 (Tyrphostin AG 1024; 2-10 μM; 1-5 days) shows a dose-dependent inhibition of cell proliferation[1].
AG1024 (1-5 μM; 1-3 days) induces UT7-9 and Baf3-p210 cells apoptosis[1].
AG1024 (2 μM; 6, 12 hours) downregulates phospho-Akt, Bcr-Abl and upregulates DNA-PKcs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:UT7-9 and Baf3-p210 cells
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Concentration:2, 5, 10 μM
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Incubation Time:1, 3, 5 days
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Result:Showed a dose-dependent inhibition of cell proliferation.
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Cell Line:UT7-9 and Baf3-p210 cells
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Concentration:1, 3, 5 μM
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Incubation Time:1, 2, 3 days
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Result:Induced apoptosis.
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Cell Line:UT7-9 and Ba/F3-p210 cells
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Concentration:2 μM
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Incubation Time:6, 12 hours
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Result:Downregulated phospho-Akt, Bcr-Abl and upregulated DNA-PKcs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female nude mice (6-8 weeks old)[1]
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Dosage:30 μg
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Administration:IP; per day; for 2 weeks
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Result:Significantly delayed the tumour growth.
Chemical Information
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CAS No. 65678-07-1
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Appearance Solid
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Molecular Weight 305.17
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Formula C14H13BrN2O
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Color White to yellow
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SMILES
N#C/C(C#N)=C\C1=CC(C(C)(C)C)=C(O)C(Br)=C1
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Synonyms
Tyrphostin AG 1024
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell Commun Signal
Megakaryocytic IGF1 coordinates activation and ferroptosis to safeguard hematopoietic stem cell regeneration after radiation injury. [Abstract]2024 May 27;22(1):292. PMID: 38802843 -
Br J Pharmacol
Targeting Na+ /K+ -ATPase by berbamine and ouabain synergizes with sorafenib to inhibit hepatocellular carcinoma. [Abstract]2021 Nov;178(21):4389-4407. PMID: 34233013 -
J Invest Dermatol
Cathelicidin Antimicrobial Peptide LL37 Induces TLR8 and Amplifies IL-36γ and IL-17C in Human Keratinocytes. [Abstract]2023 May;143(5):832-841.e4. PMID: 36496195 -
J Biol Chem
Expression of hypoxia inducible factor-dependent neuropeptide Y receptors Y1 and Y5 sensitizes hypoxic cells to NPY stimulation. [Abstract]2022 Mar;298(3):101645. PMID: 35093384 -
Pflugers Arch
Unlocking the potential: unveiling tyrphostins with Michael-reactive cyanoacrylate motif as promising inhibitors of human 5-lipoxygenase. [Abstract]2024 Dec;476(12):1913-1928. PMID: 39347835 -
Biomed Pharmacother
Insulin growth factor inhibitor as a potential new anti-schistosoma drug: An in vivo experimental study. [Abstract]2017 Nov:95:1346-1358. PMID: 28946182
AG1024 purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2017 Nov:95:1346-1358. [Abstract]
Early and late administration of AG1024 groups (C and E) shows marked collagen deposition within the granuloma compared to early and late administration of PZQ (D and F).
Solvent & Solubility
DMSO : ≥ 50 mg/mL (163.84 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Párrizas M, et al. Specific inhibition of IGF-1R and IR tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997 Apr;138(4):1427-33. [Content Brief]
[2]. Deutsch E, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation. Br J Cancer. 2004 Nov 1;91(9):1735-41. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2769 mL | 16.3843 mL | 32.7686 mL | 81.9215 mL |
| 5 mM | 0.6554 mL | 3.2769 mL | 6.5537 mL | 16.3843 mL | |
| 10 mM | 0.3277 mL | 1.6384 mL | 3.2769 mL | 8.1922 mL | |
| 15 mM | 0.2185 mL | 1.0923 mL | 2.1846 mL | 5.4614 mL | |
| 20 mM | 0.1638 mL | 0.8192 mL | 1.6384 mL | 4.0961 mL | |
| 25 mM | 0.1311 mL | 0.6554 mL | 1.3107 mL | 3.2769 mL | |
| 30 mM | 0.1092 mL | 0.5461 mL | 1.0923 mL | 2.7307 mL | |
| 40 mM | 0.0819 mL | 0.4096 mL | 0.8192 mL | 2.0480 mL | |
| 50 mM | 0.0655 mL | 0.3277 mL | 0.6554 mL | 1.6384 mL | |
| 60 mM | 0.0546 mL | 0.2731 mL | 0.5461 mL | 1.3654 mL | |
| 80 mM | 0.0410 mL | 0.2048 mL | 0.4096 mL | 1.0240 mL | |
| 100 mM | 0.0328 mL | 0.1638 mL | 0.3277 mL | 0.8192 mL |