| 中文名称: | AEE788 | ||||
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| 英文名称: | AEE788 | ||||
| 别名: | 6-[4-[(4-乙基-1-哌嗪)甲基]苯基]-N-[(1R)-1-苯基乙基]-7H-吡咯并[2,3-d]嘧啶-4-胺;AEE788 (NVP-AEE788) 抑制剂 NVP-AEE 788 | ||||
| CAS No: | 497839-62-0 | 分子式: | C27H32N6 | 分子量: | 440.58 |
| CAS No: | 497839-62-0 | ||||
| 分子式: | C27H32N6 | ||||
| 分子量: | 440.58 | ||||
基本信息
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产品编号：A11281 |
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产品名称：AEE788 |
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CAS: |
497839-62-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月 |
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分子量 |
440.58 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
88mg/mL (199.73mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内（现配现用） |
30% PEG400+0.5% Tween80+5% propylene glycol |
30mg/mL |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.2697mL |
11.3487mL |
22.6974mL |
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5mM |
0.4539mL |
2.2697mL |
4.5395mL |
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10mM |
0.2270mL |
1.1349mL |
2.2697mL |
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50mM |
0.0454mL |
0.2270mL |
0.4539mL |
生物活性
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产品描述 |
是EGFR和ErbB2的抑制剂，IC50值分别为2和6nM。 |
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靶点/IC50 |
EGFR 2nM (IC50) |
ErbB2 6nM (IC50) |
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体外研究 |
AEE788 inhibits EGFR and VEGF receptor tyrosine kinases in the nM range (IC50:EGFR 2nm, ErbB2 6nm, KDR 77nm, and Flt-1 59nm). In cells, growth factor-induced EGFR and ErbB2 phosphorylation is also efficiently inhibited (IC50:11 and 220nm, respectively). AEE788 demonstrates antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines (including EGFRvIII-dependent lines) and inhibits the proliferation of epidermal growth factor- and VEGF-stimulated human umbilical vein endothelial cells[1]. Treatment of cutaneous SCC cells with AEE788 leads to dose-dependent inhibition of EGFR and VEGFR-2 phosphorylation, growth inhibition, and induction of apoptosis. |
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体内研究 |
AEE788 efficiently inhibits growth factor-induced EGFR and ErbB2 phosphorylation in tumors for >72h. AEE788 also inhibits VEGF-induced angiogenesis in a murine implant model. In mice treated with AEE788, tumor growth is inhibited by 54% at 21days after the start of treatment compared with control mice. |
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推荐实验方法(仅供参考)
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激酶实验： |
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The invitro kinase assays are performed in 96-well plates (30μL) at ambient temperature for 15–45 min using the recombinant glutathione S-transferase-fused kinase domains (4–100ng, depending on specific activity). [γ33P]ATP is used as phosphate donor and polyGluTyr-(4:1) peptide as acceptor. Assays are optimized for each kinase using the following ATP concentrations: 1.0μM (c-Kit, c-Met, c-Fms, c-Raf-1, and RET), 2.0μM (EGFR, ErbB2, ErbB3, and ErbB4), 5.0μM (c-Abl), 8.0μM (Flt-1, Flt-3, Flt-4, Flk, KDR, FGFR-1, and Tek), 10.0μM (PDG receptor-β, protein kinase C-α, and cyclin-dependent kinase 1),and 20.0μM (c-Src and protein kinase A). The reaction is terminated by the addition of 20μL 125mM EDTA. ThirtyμL (c-Abl,c-Src, insulin-like growth factor-1R, RET-Men2A, and RET-Men2B) or 40μL (all other kinases) of the reaction mixture is transferred onto Immobilon-polyvinylidene difluoride membrane, presoaked with 0.5% H3PO4 and mounted on a vacuum manifold. Vacuum is then applied and each well rinsed with 200μL 0.5% H3PO4. Membranes are removed and washed four times. Dried membranes are counted. IC50 are calculated by linear regression analysis of the percentage inhibition and are averages of at least three determinations |
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细胞实验: |
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AEE788 is dissolved in 90% polyethylene glycol 300 plus 10% 1-methyl-2-pyrrolidinone to a concentration of 6.25mg/mL.Tumor cells are seeded into 96-well plates in complete medium and allowed to attach for 24hours. The cultures are re-fed with medium with 2% serum. After 24hours, cells are treated with different concentrations (0-2μM) of AEE788 (negative control with DMSO alone) for 72hours. After a 2-hour incubation in medium containing 0.42mg/mL MTT, the cells are lysed in 100μL DMSO. The conversion of MTT to formazan is measured at an absorbance of 570nm |
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动物实验: |
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Mice: AEE788 is diluted in DMSO and diluted in the optimal medium. BALB/c mice bearing s.c. A-431 squamous tumors (3animals/group) or HC11-NeuT-driven breast tumors (2 animals/group) are dosed orally with 30mg/kg of AEE788 or vehicle once daily for 5days. At different time points after the end of compound treatment and before sacrificing the animals the mice are given i.v. 500μg EGF/kg body weight or 0.2ml 0.9% w/v NaCl as vehicle control. Five min after EGF administration,the mice are sacrificed, tumors are removed |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
