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AEE788 (NVP-AEE788) is a novel multitargeted human epidermal receptor (HER) 1/2 and vascular endothelial growth factor receptor (VEGFR) 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1. In cells, growth factor-induced EGFR and ErbB2 phosphorylation was also efficiently inhibited with IC50s of 11 and 220 nM, respectively. It efficiently inhibited growth factor-induced EGFR and ErbB2 phosphorylation in tumors for >72 h, a phenomenon correlating with the antitumor efficacy of intermittent treatment schedules. AEE788 also inhibits VEGF-induced angiogenesis in a murine implant model. It has potential as an anticancer agent targeting deregulated tumor cell proliferation as well as angiogenic parameters.
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Source | PLoS One (2017). Figure 4. AEE788 |
| Method | Western blot analyses | |
| Cell Lines | TGCT cell lines | |
| Concentrations | 30 nM | |
| Incubation Time | 24 h | |
| Results | Interestingly, treatment with AEE788 also led to a decreased activation of mTOR in some cell lines |
| Cell Experiment | |
|---|---|
| Cell lines | NCI-H596, BT-474, SK-BR-3, 32D/EGFR, T24, MCF-7 and MCF-7/EGFRvII cells |
| Preparation method | Endothelial Cell Proliferation Assay. To test the effects of AEE788 on serum, VEGF, EGF, and basic fibroblast growth factor (bFGF)-induced proliferation of human umbilical vein endothelial cells an endothelial cell proliferation assay, based on BrdUrd incorporation, was used as already. |
| Concentrations | 0~10µM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | mouse xenografts models NCI-H596 and DU145 tumors |
| Formulation | N-methylpyrrolidone and PEG300 1:9 (v/v) |
| Dosages | 7.5, 15, 30, 50mg/kg *3days weekly for 35 days |
| Administration | p.o. |
| Molecular Weight | 440.58 |
| Formula | C27H32N6 |
| CAS Number | 497839-62-0 |
| Solubility (25°C) | DMSO ≥ 65 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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