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Submit ReviewAEE 788 is a potent EGFR and VEGFR inhibitor (IC50 values are 2, 6, 59, 77, 160 and 330 nM for EGFR, ErbB2, VEGFR-1, VEGFR-2, ErbB4 and VEGFR-3 respectively). Also inhibits c-Abl, c-Fms and c-Src (IC50 values are 52, 60 and 61 nM respectively). Inhibits proliferation of EGFR and ErbB2 overexpressing cancer cell lines in vitro. Inhibits tumor xenograft growth and VEGF-induced angiogenesis in mice. Orally active.
分子量 | 440.58 |
公式 | C27H32N6 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 497839-62-0 |
PubChem ID | 10297043 |
InChI Key | OONFNUWBHFSNBT-HXUWFJFHSA-N |
Smiles | C[C@@H](NC2=C(C=C(C4=CC=C(CN5CCN(CC)CC5)C=C4)N3)C3=NC=N2)C1=CC=CC=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 44.06 | 100 |
以下数据基于产品分子量 440.58。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.27 mL | 11.35 mL | 22.7 mL |
5 mM | 0.45 mL | 2.27 mL | 4.54 mL |
10 mM | 0.23 mL | 1.13 mL | 2.27 mL |
50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
参考文献是支持产品生物活性的出版物。
Traxler et al (2004) AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 64 4931 PMID: 15256466
Yokoi et al (2005) Dual inhibition of epidermal growth factor receptor and vascular endothelial growth factor receptor phosphorylation by AEE788 reduces growth and metastasis of human colon carcinoma in an orthotopic nude mouse model. Cancer Res. 65 3716 PMID: 15867367
If you know of a relevant reference for AEE 788, please let us know.
关键词: AEE 788, AEE 788 supplier, AEE788, potent, epidermal, vascular, endothelial, growth, factors, EGFR, VEGFR, ErbB2, antiangiogenic, antitumor, orally, active, 5318, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AEE 788 的部分引用包括:
Bill et al (2015) ANO1 interacts with EGFR and correlates with sensitivity to EGFR-targeting therapy in head and neck cancer. Int J Mol Sci 6 9173 PMID: 25823819
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平均评分: 5 (基于 2 条评论。)
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Used this to inhibit proliferation, looks great!
Used in vitro to investigate ERG pathway in connection with VGEF