| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 1 µM (PI5P4Kα) | ||||||||||||
| Invitro | 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: | ||||||||||||
| Name | I-OMe-Tyrphostin AG 538 | ||||||||||||
| CAS | 1094048-77-7 | ||||||||||||
| Formula | C17H12INO5 | ||||||||||||
| Molar Mass | 437.19 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. [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. |