Date published: 2025-10-2

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AG 1024 (CAS 65678-07-1)

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See product citations (22)

Alternate Names:
Tyrphostin AG 1024
Application:
AG 1024 is inhibits insulin-stimulated cellular proliferation and IGF-1R autophosphorylation
CAS Number:
65678-07-1
Purity:
≥98%
Molecular Weight:
305.17
Molecular Formula:
C14H13BrN2O
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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AG 1024 selectively inhibits the IGF-1R (insulin-like growth factor 1 receptor). Human breast cancer cell studies report AG 1024 to induce apoptosis, inhibit cell proliferation, decrease bcl-2 and phospho-Akt1 expression, and elevate the expression levels of Bax, p53 and p21. Studies report AG 1024 to block tyrosine kinase activity and to have a lower IC50 for IGF-1 in comparison to insulin receptors. Other studies indicate that exposure of SHR cells to AG 1024 decreases Ang II-mediated NAD(P)H oxidase activation. AG 1024 is an inhibitor of insulin R.


AG 1024 (CAS 65678-07-1) References

  1. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells.  |  Wen, B., et al. 2001. Br J Cancer. 85: 2017-21. PMID: 11747348
  2. Vascular smooth muscle cell NAD(P)H oxidase activity during the development of hypertension: Effect of angiotensin II and role of insulinlike growth factor-1 receptor transactivation.  |  Cruzado, MC., et al. 2005. Am J Hypertens. 18: 81-7. PMID: 15691621
  3. P2Y12 receptor signalling towards PKB proceeds through IGF-I receptor cross-talk and requires activation of Src, Pyk2 and Rap1.  |  Van Kolen, K., et al. 2006. Cell Signal. 18: 1169-81. PMID: 16236484
  4. Permissive role of insulin in the expression of long-term potentiation in the hippocampus of immature rats.  |  Zhao, W., et al. 2010. Neurosignals. 18: 236-45. PMID: 21346324
  5. Cross-talk between insulin and IGF-1 receptors in the cortical collecting duct principal cells: implication for ENaC-mediated Na+ reabsorption.  |  Ilatovskaya, DV., et al. 2015. Am J Physiol Renal Physiol. 308: F713-9. PMID: 25651558
  6. Insulin treatment promotes tyrosine phosphorylation of PKR and inhibits polyIC induced PKR threonine phosphorylation.  |  Swetha, M. and Ramaiah, KVA. 2015. Arch Biochem Biophys. 585: 98-108. PMID: 26321373
  7. Activation of the IGF1R pathway potentially mediates acquired resistance to mutant-selective 3rd-generation EGF receptor tyrosine kinase inhibitors in advanced non-small cell lung cancer.  |  Park, JH., et al. 2016. Oncotarget. 7: 22005-15. PMID: 26980747
  8. Relative expression of the p75 neurotrophin receptor, tyrosine receptor kinase A, and insulin receptor in SH-SY5Y neuroblastoma cells and hippocampi from Alzheimer's disease patients.  |  Ito, S., et al. 2016. Neurochem Int. 101: 22-29. PMID: 27693452
  9. Genistein and AG1024 synergistically increase the radiosensitivity of prostate cancer cells.  |  Tang, Q., et al. 2018. Oncol Rep. 40: 579-588. PMID: 29901146
  10. AG-1024 Sensitizes Sorafenib-Resistant Hepatocellular Carcinoma Cells to Sorafenib via Enhancing G1/S Arrest.  |  Zhou, W., et al. 2021. Onco Targets Ther. 14: 1049-1059. PMID: 33623392
  11. Triptolide prevents LPS-induced skeletal muscle atrophy via inhibiting NF-κB/TNF-α and regulating protein synthesis/degradation pathway.  |  Fang, WY., et al. 2021. Br J Pharmacol. 178: 2998-3016. PMID: 33788266
  12. Tyrphostin AG1024 downregulates aryl hydrocarbon receptor (AhR) expression in an IGF1R and IR-independent manner.  |  Tomita, S., et al. 2022. Toxicol Lett. 360: 62-70. PMID: 35149128
  13. Tyrphostin AG1024 Suppresses Coronaviral Replication by Downregulating JAK1 via an IR/IGF-1R Independent Proteolysis Mediated by Ndfip1/2_NEDD4-like E3 Ligase Itch.  |  Yang, CW., et al. 2022. Pharmaceuticals (Basel). 15: PMID: 35215353
  14. AG1024, an IGF-1 receptor inhibitor, ameliorates renal injury in rats with diabetic nephropathy via the SOCS/JAK2/STAT pathway.  |  Liu, J., et al. 2023. Open Med (Wars). 18: 20230683. PMID: 37034500
  15. Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins.  |  Párrizas, M., et al. 1997. Endocrinology. 138: 1427-33. PMID: 9075698

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

AG 1024, 1 mg

sc-205907
1 mg
$105.00