I-OMe-Tyrphostin AG 538

Modify Date: 2025-08-26 12:36:23

I-OMe-Tyrphostin AG 538 Structure
I-OMe-Tyrphostin AG 538 structure
Common Name I-OMe-Tyrphostin AG 538
CAS Number 1094048-77-7 Molecular Weight 437.19
Density N/A Boiling Point N/A
Molecular Formula C17H12INO5 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of I-OMe-Tyrphostin AG 538


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].

 Names

Name I-OMe-Tyrphostin AG 538

 I-OMe-Tyrphostin AG 538 Biological Activity

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].
Related Catalog
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]. 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.
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.

[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.

 Chemical & Physical Properties

Molecular Formula C17H12INO5
Molecular Weight 437.19
InChIKey HSRMHXWCTRFVHK-NYYWCZLTSA-N
SMILES COc1cc(C=C(C#N)C(=O)c2ccc(O)c(O)c2)cc(I)c1O

 Safety Information

Hazard Codes Xi
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