For research use only. Not for therapeutic Use.
AEE-788 (Cat.No:I003750) is a small-molecule inhibitor of epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR) tyrosine kinases. It is being studied as a potential treatment for various types of cancer. AEE-788 has shown promising results in preclinical studies and is currently undergoing clinical trials to assess its safety and efficacy.
| Catalog Number | I003750 |
| CAS Number | 497839-62-0 |
| Synonyms | 6-[4-[(4-ethylpiperazin-1-yl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine |
| Molecular Formula | C₂₇H₃₂N₆ |
| Purity | ≥95% |
| Target | EGFR |
| Solubility | DMSO 88 mg/mL; Water <1 mg/mL; Ethanol <1 mg/mL |
| Storage | 3 years -20℃ powder |
| IC50 | 2 nM( EGFR); 6 nM (ErbB2) [1] |
| InChI | InChI=1S/C27H32N6/c1-3-32-13-15-33(16-14-32)18-21-9-11-23(12-10-21)25-17-24-26(28-19-29-27(24)31-25)30-20(2)22-7-5-4-6-8-22/h4-12,17,19-20H,3,13-16,18H2,1-2H3,(H2,28,29,30,31)/t20-/m1/s1 |
| InChIKey | OONFNUWBHFSNBT-HXUWFJFHSA-N |
| SMILES | CCN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(N3)N=CN=C4NC(C)C5=CC=CC=C5 |
| Reference | </br>1:AEE788 Inhibits Basal Body Assembly and Blocks DNA Replication in the African Trypanosome. Sullenberger C, Piqué D, Ogata Y, Mensa-Wilmot K.Mol Pharmacol. 2017 May;91(5):482-498. doi: 10.1124/mol.116.106906. Epub 2017 Feb 28. PMID: 28246189 </br>2:Using pharmacokinetic and pharmacodynamic data in early decision making regarding drug development: a phase I clinical trial evaluating tyrosine kinase inhibitor, AEE788. Baselga J, Mita AC, Schöffski P, Dumez H, Rojo F, Tabernero J, DiLea C, Mietlowski W, Low C, Huang J, Dugan M, Parker K, Walk E, van Oosterom A, Martinelli E, Takimoto CH.Clin Cancer Res. 2012 Nov 15;18(22):6364-72. doi: 10.1158/1078-0432.CCR-12-1499. Epub 2012 Sep 26. PMID: 23014528 Free Article</br>3:AEE788 potentiates celecoxib-induced growth inhibition and apoptosis in human colon cancer cells. Venkatesan P, Bhutia SK, Singh AK, Das SK, Dash R, Chaudhury K, Sarkar D, Fisher PB, Mandal M.Life Sci. 2012 Oct 22;91(15-16):789-99. doi: 10.1016/j.lfs.2012.08.024. Epub 2012 Aug 24. PMID: 22922496 </br>4:Phase I study of AEE788, a novel multitarget inhibitor of ErbB- and VEGF-receptor-family tyrosine kinases, in recurrent glioblastoma patients. Reardon DA, Conrad CA, Cloughesy T, Prados MD, Friedman HS, Aldape KD, Mischel P, Xia J, DiLea C, Huang J, Mietlowski W, Dugan M, Chen W, Yung WK.Cancer Chemother Pharmacol. 2012 Jun;69(6):1507-18. doi: 10.1007/s00280-012-1854-6. Epub 2012 Mar 7. PMID: 22392572 Free PMC Article</br>5:Pharmacokinetic drug interaction between AEE788 and RAD001 causing thrombocytopenia in patients with glioblastoma. Reardon DA, Cloughesy T, Rich J, Alfred Yung WK, Yung L, DiLea C, Huang J, Dugan M, Mietlowski W, Maes A, Conrad C.Cancer Chemother Pharmacol. 2012 Jan;69(1):281-7. doi: 10.1007/s00280-011-1754-1. Epub 2011 Oct 9. PMID: 21984222 </br>6:Dual Inhibitor AEE788 Reduces Tumor Growth in Preclinical Models of Medulloblastoma. Meco D, Servidei T, Zannoni GF, Martinelli E, Prisco MG, de Waure C, Riccardi R.Transl Oncol. 2010 Oct 1;3(5):326-35. PMID: 20885895 Free PMC Article</br>7:Effect of additional inhibition of human epidermal growth factor receptor 2 with the bispecific tyrosine kinase inhibitor AEE788 on the resistance to specific EGFR inhibition in glioma cells. Berezowska S, Diermeier-Daucher S, Brockhoff G, Busch R, Duyster J, Grosu AL, Schlegel J.Int J Mol Med. 2010 Nov;26(5):713-21. PMID: 20878094 </br>8:EGFR/HER2 inhibitor AEE788 increases ER-mediated transcription in HER2/ER-positive breast cancer cells but functions synergistically with endocrine therapy. Evans AH, Pancholi S, Farmer I, Thornhill A, Evans DB, Johnston SR, Dowsett M, Martin LA.Br J Cancer. 2010 Apr 13;102(8):1235-43. doi: 10.1038/sj.bjc.6605641. PMID: 20386540 Free PMC Article</br>9:AEE788 is a vascular endothelial growth factor receptor tyrosine kinase inhibitor with antiproliferative and proapoptotic effects in acute myeloid leukemia. Barbarroja N, Torres LA, Rodriguez-Ariza A, Valverde-Estepa A, Lopez-Sanchez LM, Ruiz-Limon P, Perez-Sanchez C, Carretero RM, Velasco F, López-Pedrera C.Exp Hematol. 2010 Aug;38(8):641-52. doi: 10.1016/j.exphem.2010.03.017. Epub 2010 Apr 7. PMID: 20380868 </br>10:The anti-proliferative side effects of AEE788, a tyrosine kinase inhibitor blocking both EGF- and VEGF-receptor, are liver-size-dependent after partial hepatectomy in rats. Deng M, Huang H, Jin H, Dirsch O, Dahmen U.Invest New Drugs. 2011 Aug;29(4):593-606. doi: 10.1007/s10637-010-9394-6. Epub 2010 Feb 12. PMID: 20148349 |
