I-OMe-Tyrphostin AG 538
Based on 1 publication(s) in Google Scholar
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells.?I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50?of 1 μM.
For research use only. We do not sell to patients.
- Purity: 98.03%
- CAS No.: 1094048-77-7
- Formula: C17H12INO5
- Molecular Weight:437.19
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) I-OMe-Tyrphostin AG 538
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Biological Activity
IC50: 1 µM (PI5P4Kα)[1]
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) (0.1-1000 μM; 24 hours) is cytotoxic to PANC-1 cells in nutrient-deprived medium[1].
I-OMe-Tyrphostin AG 538 (0-3 μM; 1 hour) blocks phosphorylation of IGF-1R, Akt and Erk[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PANC-1 cells
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Concentration:0.1, 1, 10, 1000 µM
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Incubation Time:24 hours
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Result:Cytotoxic to PANC-1 cells in nutrient-deprived medium.
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Cell Line:PANC-1 cells (stimulation with 50 ng/ml IGF-1 for 10 min)
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Concentration:0.03, 0.3, 3 µM
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Incubation Time:1 hour
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Result:Blocked phosphorylation of IGF-1R, Akt and Erk.
Chemical Information
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CAS No. 1094048-77-7
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Appearance Solid
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Molecular Weight 437.19
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Formula C17H12INO5
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Color Yellow to orange
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SMILES
N#C/C(C(C1=CC=C(O)C(O)=C1)=O)=C\C2=CC(OC)=C(O)C(I)=C2
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Synonyms
I-OMe-AG 538
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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 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cancer Res
An Immune Subtype Classification System Enables the Development of Strategies to Predict and Enhance Immunotherapy Responses in Colorectal Cancer. [Abstract]2025 Apr 15;85(8):1441-1458. PMID: 39879113
Solvent & Solubility
DMSO : 50 mg/mL (114.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (5.72 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.72 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Davis MI, et al. A homogeneous, high-throughput assay for phosphatidylinositol 5-phosphate 4-kinase with a novel, rapid substrate preparation. PLoS One. 2013;8(1):e54127. [Content Brief]
[2]. Momose I, et al. Inhibitors of insulin-like growth factor-1 receptor tyrosine kinase are preferentially cytotoxic to nutrient-deprived pancreatic cancer cells. Biochem Biophys Res Commun. 2009 Feb 27;380(1):171-6. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2873 mL | 11.4367 mL | 22.8734 mL | 57.1834 mL |
| 5 mM | 0.4575 mL | 2.2873 mL | 4.5747 mL | 11.4367 mL | |
| 10 mM | 0.2287 mL | 1.1437 mL | 2.2873 mL | 5.7183 mL | |
| 15 mM | 0.1525 mL | 0.7624 mL | 1.5249 mL | 3.8122 mL | |
| 20 mM | 0.1144 mL | 0.5718 mL | 1.1437 mL | 2.8592 mL | |
| 25 mM | 0.0915 mL | 0.4575 mL | 0.9149 mL | 2.2873 mL | |
| 30 mM | 0.0762 mL | 0.3812 mL | 0.7624 mL | 1.9061 mL | |
| 40 mM | 0.0572 mL | 0.2859 mL | 0.5718 mL | 1.4296 mL | |
| 50 mM | 0.0457 mL | 0.2287 mL | 0.4575 mL | 1.1437 mL | |
| 60 mM | 0.0381 mL | 0.1906 mL | 0.3812 mL | 0.9531 mL | |
| 80 mM | 0.0286 mL | 0.1430 mL | 0.2859 mL | 0.7148 mL | |
| 100 mM | 0.0229 mL | 0.1144 mL | 0.2287 mL | 0.5718 mL |
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