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I-OMe-Tyrphostin AG 538

Alias: IOMeTyrphostin AG 538; I OMe Tyrphostin AG 538
Cat No.:V40006 Purity: ≥98%
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R kinase.
I-OMe-Tyrphostin AG 538
I-OMe-Tyrphostin AG 538 Chemical Structure CAS No.: 1094048-77-7
Product category: New2
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
50mg
Other Sizes
Official Supplier of:
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Product Description
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R kinase. I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-starved PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive PI5P4Kα inhibitor (antagonist) with IC50 of 1 μM.
Biological Activity I Assay Protocols (From Reference)
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].
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.
References

[1]. A homogeneous, high-throughput assay for phosphatidylinositol 5-phosphate 4-kinase with a novel, rapid substrate preparation. PLoS One. 2013;8(1):e54127.

[2]. 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.

Additional Infomation
2-[(3,4-dihydroxyphenyl)-oxomethyl]-3-(4-hydroxy-3-iodo-5-methoxyphenyl)-2-propenenitrile is a member of chalcones.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H12INO5
Molecular Weight
437.185357093811
Exact Mass
436.976
CAS #
1094048-77-7
PubChem CID
5353685
Appearance
Yellow to orange solid powder
LogP
3.2
Hydrogen Bond Donor Count
3
Hydrogen Bond Acceptor Count
6
Rotatable Bond Count
4
Heavy Atom Count
24
Complexity
542
Defined Atom Stereocenter Count
0
SMILES
IC1C(=C(C=C(C=1)C=C(C#N)C(C1C=CC(=C(C=1)O)O)=O)OC)O
InChi Key
HSRMHXWCTRFVHK-NYYWCZLTSA-N
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+
Chemical Name
(E)-2-(3,4-dihydroxybenzoyl)-3-(4-hydroxy-3-iodo-5-methoxyphenyl)prop-2-enenitrile
Synonyms
IOMeTyrphostin AG 538; I OMe Tyrphostin AG 538
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~50 mg/mL (~114.37 mM)
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.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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