I-OMe-Tyrphostin AG 538

• CAT Number: I016849
• CAS Number: 1094048-77-7
• Molecular Formula: C17H12INO5
• Molecular Weight: 437.19
• Purity: ≥95%
• Synonyms: (E)-2-(3,4-dihydroxybenzoyl)-3-(4-hydroxy-3-iodo-5-methoxyphenyl)prop-2-enenitrile
• InChI: 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+
• InChIKey: HSRMHXWCTRFVHK-NYYWCZLTSA-N
• SMILES: COC1=C(C(=CC(=C1)C=C(C#N)C(=O)C2=CC(=C(C=C2)O)O)I)O

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].
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].

Reference

[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]