AEE-788 is an inhibitor of EGFR, HER2, VEGFR2, and FLT3 that exhibits anticancer chemotherapeutic activity. In animal models with ependymoma xenografts, AEE-788 increases survival rates. In acute myelogenous leukemia (AML) cells, AEE-788 inhibits cell proliferation and induces apoptosis. This compound displays mixed results in a clinical setting due to high toxicity.
| Cas No. | 497839-62-0 |
|---|---|
| Purity | ≥98% |
| Formula | C27H32N6 |
| Formula Wt. | 440.60 |
| IUPAC Name | 6-{4-[(4-Ethyl-1-piperazinyl)methyl]phenyl}-N-[(1R)-1-phenylethyl]-1H-pyrrolo[2,3-d]pyrimidin-4-amine |
| Synonym | AEE788, NVP-AEE788 |
| Solubility | 100mM in DMSO insoluble in ethanol and H2O |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | |
|---|---|
| Info Sheet |
Baselga J, Mita AC, Schöffski P, et al. Using pharmacokinetic and pharmacodynamic data in early decision making regarding drug development: a phase I clinical trial evaluating tyrosine kinase inhibitor, AEE788. Clin Cancer Res. 2012 Nov 15;18(22):6364-72. PMID: 23014528.
Servidei T, Meco D, Trivieri N, et al. Effects of epidermal growth factor receptor blockade on ependymoma stem cells in vitro and in orthotopic mouse models. Int J Cancer. 2012 Sep 1;131(5):E791-803. PMID: 22120695.
Reardon DA, Conrad CA, Cloughesy T, et al. Phase I study of AEE788, a novel multitarget inhibitor of ErbB- and VEGF-receptor-family tyrosine kinases, in recurrent glioblastoma patients. Cancer Chemother Pharmacol. 2012 Jun;69(6):1507-18. PMID: 22392572.
Barbarroja N, Torres LA, Rodriguez-Ariza A, et al. AEE788 is a vascular endothelial growth factor receptor tyrosine kinase inhibitor with antiproliferative and proapoptotic effects in acute myeloid leukemia. Exp Hematol. 2010 Aug;38(8):641-52. PMID: 20380868.
