1. Protein Tyrosine Kinase/RTK
  2. IGF-1R
  3. I-OMe-Tyrphostin AG 538

I-OMe-Tyrphostin AG 538 (Synonyms: I-OMe-AG 538)

Cat. No.: HY-135680 Purity: 99.34%
Handling Instructions

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.

I-OMe-Tyrphostin AG 538 Chemical Structure

I-OMe-Tyrphostin AG 538 Chemical Structure

CAS No. : 1094048-77-7

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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target

IC50: 1 µM (PI5P4Kα)[1]

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: PANC-1 cells
Concentration: 0.1, 1, 10, 1000 µM
Incubation Time: 24 hours
Result: Cytotoxic to PANC-1 cells in nutrient-deprived medium.

Western Blot Analysis[1]

Cell Line: PANC-1 cells (stimulation with 50 ng/ml IGF-1 for 10 min)
Concentration: 0.03, 0.3, 3 µM
Incubation Time: 1 hour
Result: Blocked phosphorylation of IGF-1R, Akt and Erk.
Molecular Weight

437.19

Formula

C17H12INO5

CAS No.
SMILES

N#C/C(C(C1=CC=C(O)C(O)=C1)=O)=C\C2=CC(OC)=C(O)C(I)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (114.37 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Product Name:
I-OMe-Tyrphostin AG 538
Cat. No.:
HY-135680
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