AG-1024 is a selective IGF-1R kinase inhibitor with modest activity. It inhibits insulin-stimulated cellular proliferation with IC50 of 0.4 µM. [1] AG-1024 showed synergistic effect with irradation and inhibited proliferation and induced apoptosis in human breast cancer MCF-7 cells. [2] AG-1024 also inhibited autocrine growth of human prostate cancer DU145 cells with an IC50 value of 2.5 µM.[3]In vivo, daily administration of AG-1024 through i.v. route at 1-2 mg/kg has been shown to increase the survival rate of mouse injected with Ba/F3-p210 cells. [4]
Technical information:
| Chemical Formula: | C14H13BrN2O | |
| CAS #: | 65678-07-1 | |
| Molecular Weight: | 305.17 | |
| Purity: | > 98% | |
| Appearance: | Orange | |
| Chemical Name: | 2-(3-bromo-5-(tert-butyl)-4-hydroxybenzylidene)malononitrile | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | AG1024, AG 1024, Tyrphostin AG-1024, |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.
Reference:
| 1. | Párrizas M, et al. Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997; 138(4):1427-33. Pubmed ID:9075698 |
| 2. | Wen B, et al. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells. Br J Cancer. 2001; 85(12):2017-21. Pubmed ID:11747348 |
| 3. | Kisielewska J, et al. The effect of tyrosine kinase inhibitors, tyrphostins: AG1024 and SU1498, on autocrine growth of prostate cancer cells (DU145). Folia Histochem Cytobiol. 2008; 46(2):185-91. Pubmed ID:18519236 |
| 4. | Deutsch E, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation. Br J Cancer. 2004; 91(9):1735-41. Pubmed ID:11747348 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
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