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1094048-77-7

1094048-77-7 structure
1094048-77-7 structure
  • Name: I-OMe-Tyrphostin AG 538
  • Chemical Name: I-OMe-Tyrphostin AG 538
  • CAS Number: 1094048-77-7
  • Molecular Formula: C17H12INO5
  • Molecular Weight: 437.19
  • Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK IGF-1R
  • Create Date: 2020-04-13 23:05:34
  • Modify Date: 2024-01-12 10:17:29
  • 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].

Name I-OMe-Tyrphostin AG 538
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.

Molecular Formula C17H12INO5
Molecular Weight 437.19
Hazard Codes Xi