| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
I-OMe-Tyrphostin AG 538 targets insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase and PI5P4Kα (phosphatidylinositol-5-phosphate 4-kinase type-2 alpha). IGF-1R is a receptor tyrosine kinase that mediates the effects of insulin-like growth factor-1 (IGF-1) on cell growth, proliferation, and survival. Overexpression or hyperactivation of IGF-1R is associated with various cancers, making it an important therapeutic target. PI5P4Kα is a lipid kinase involved in phosphoinositide metabolism and cell signaling. I-OMe-Tyrphostin AG 538 is a specific inhibitor of IGF-1R kinase and an ATP-competitive inhibitor of PI5P4Kα with an IC₅₀ of 1 µM.
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| ln Vitro |
To PANC-1 cells in culture medium, I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) (0.1-1000 μM; 24 hours) is cytotoxic [1].
In vitro, I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and exhibits preferential cytotoxicity to nutrient-deprived PANC1 pancreatic cancer cells. Strong effects are observed at 0.1-1000 μM over 24 hours. The compound's preferential cytotoxicity to nutrient-deprived cells suggests that it may target metabolic vulnerabilities in cancer cells. I-OMe-Tyrphostin AG 538 is used as a cell signaling inhibitor in PC-1 cell lines and in high-throughput screening assays for IGF1R inhibitors. Its activity is concentration-dependent, with efficacy observed across a broad range of concentrations. |
| ln Vivo |
In vivo, I-OMe-Tyrphostin AG 538 has not been extensively reported in the available literature. As an inhibitor of IGF-1R and PI5P4Kα, the compound may have potential applications in cancer therapy. IGF-1R inhibitors have been studied in various preclinical models for their anti-tumor activity. The compound's preferential cytotoxicity to nutrient-deprived PANC1 cells suggests potential for targeting pancreatic cancer, a disease characterized by nutrient deprivation and metabolic stress. However, detailed in vivo efficacy, pharmacokinetic, and toxicological data for I-OMe-Tyrphostin AG 538 require further investigation from primary research publications.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cellular) assays for I-OMe-Tyrphostin AG 538 involve measuring inhibition of IGF-1R kinase activity or PI5P4Kα activity using purified recombinant enzymes. For IGF-1R kinase assays, the enzyme is incubated with varying concentrations of the compound, ATP, and a peptide substrate. Phosphorylation of the substrate is detected using radioactive (³³P-ATP) or fluorescence-based methods. IC₅₀ values are calculated from concentration-response curves. For PI5P4Kα assays, the enzyme is incubated with the compound, ATP, and phosphatidylinositol-5-phosphate (PI5P). The production of phosphatidylinositol-4,5-bisphosphate (PI4,5P₂) is measured using radiometric or lipid-based assays. The compound's IC₅₀ of 1 µM for PI5P4Kα is determined using these assays.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: PANC-1 cells Tested Concentrations: 0.1, 1, 10, 1000 µM Incubation Time (0-3 µM; 1 hour) Inhibits the phosphorylation of IGF-1R, Akt and Erk[1]. Incubation Duration: 24 hour Experimental Results: Cytotoxic to PANC-1 cells in nutrient-poor medium. Western Blot Analysis [1] Cell Types: PANC-1 cells (stimulated with 50 ng/ml IGF-1 for 10 minutes) Tested Concentrations: 0.03, 0.3, 3 µM Incubation Duration: 1 hour Experimental Results: Phosphorylation of IGF-1R, Akt was Block and Elk. In vitro cellular experiments with I-OMe-Tyrphostin AG 538 are performed using PANC1 pancreatic cancer cells or other cancer cell lines. Cells are cultured in appropriate media under normal or nutrient-deprived conditions (e.g., glucose-free or serum-free media) and treated with varying concentrations of the compound (0.1-1000 μM) for 24 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. IGF-1R-mediated signaling is assessed by measuring the phosphorylation of IGF-1R and downstream targets (e.g., AKT, ERK) using Western blot analysis with phospho-specific antibodies. The compound's preferential cytotoxicity to nutrient-deprived cells is a key endpoint. |
| Animal Protocol |
In vivo animal studies with I-OMe-Tyrphostin AG 538 have not been extensively reported. For pancreatic cancer studies, standard in vivo models include xenografts of PANC1 or other pancreatic cancer cell lines in immunocompromised mice. Mice are injected with cancer cells via subcutaneous or orthotopic implantation, and after tumor establishment, treated with I-OMe-Tyrphostin AG 538 via oral, intraperitoneal, or intravenous administration at various doses and schedules. Efficacy is assessed by measuring tumor volume, weight, and histopathological examination. Pharmacodynamic markers such as IGF-1R phosphorylation and downstream signaling may be measured to confirm target engagement.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of I-OMe-Tyrphostin AG 538 are not extensively characterized. The compound has a molecular weight of approximately 400-500 (exact molecular weight not specified in search results) and is a tyrphostin derivative. As a small molecule, it is expected to have reasonable oral bioavailability and cellular permeability. Storage: follow manufacturer's guidelines. Detailed pharmacokinetic parameters including half-life, clearance, and bioavailability require further investigation from primary research publications.
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| Toxicity/Toxicokinetics |
Toxicological information for I-OMe-Tyrphostin AG 538 is not extensively detailed in the available literature. As a research compound with kinase inhibitory activity, it should be handled with appropriate safety precautions. Standard safety guidelines for handling potent pharmaceutical compounds apply, including use of personal protective equipment (gloves, safety goggles, lab coat), working in a well-ventilated area, and proper chemical waste disposal. The compound is intended for research use only and is not approved for human therapeutic use. Cytotoxicity studies in cell-based assays help establish the therapeutic window and selectivity index of the compound.
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| References |
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| Additional Infomation |
2-[(3,4-dihydroxyphenyl)-oxymethyl]-3-(4-hydroxy-3-iodo-5-methoxyphenyl)-2-acrylonitrile is a chalcone compound.
I-OMe-Tyrphostin AG 538 (CAS 1094048-77-7) is a specific inhibitor of insulin-like growth factor-1 receptor (IGF-1R) tyrosine kinase and an ATP-competitive inhibitor of PI5P4Kα with an IC₅₀ of 1 µM. The compound inhibits IGF-1R-mediated signaling and exhibits preferential cytotoxicity to nutrient-deprived PANC1 pancreatic cancer cells. Strong effects are observed at 0.1-1000 μM over 24 hours. I-OMe-Tyrphostin AG 538 is also known as I-OMe-AG 538 and is used as a cell signaling inhibitor in PC-1 cell lines and in high-throughput screening assays for IGF1R inhibitors. |
| Molecular Formula |
C17H12INO5
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|---|---|
| Molecular Weight |
437.185357093811
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| Exact Mass |
436.976
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| CAS # |
1094048-77-7
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| PubChem CID |
5353685
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| Appearance |
Yellow to orange solid powder
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| LogP |
3.2
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
542
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| Defined Atom Stereocenter Count |
0
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| SMILES |
IC1C(=C(C=C(C=1)C=C(C#N)C(C1C=CC(=C(C=1)O)O)=O)OC)O
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| InChi Key |
HSRMHXWCTRFVHK-NYYWCZLTSA-N
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| InChi Code |
InChI=1S/C17H12INO5/c1-24-15-6-9(5-12(18)17(15)23)4-11(8-19)16(22)10-2-3-13(20)14(21)7-10/h2-7,20-21,23H,1H3/b11-4+
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| Chemical Name |
(E)-2-(3,4-dihydroxybenzoyl)-3-(4-hydroxy-3-iodo-5-methoxyphenyl)prop-2-enenitrile
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| Synonyms |
IOMeTyrphostin AG 538; I OMe Tyrphostin AG 538
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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) |
DMSO : ~50 mg/mL (~114.37 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.72 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2873 mL | 11.4367 mL | 22.8734 mL | |
| 5 mM | 0.4575 mL | 2.2873 mL | 4.5747 mL | |
| 10 mM | 0.2287 mL | 1.1437 mL | 2.2873 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.
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