化合物 AEE788|T2116|TargetMol

AEE788
497839-62-0

￥283 1mg 起订

￥395 2mg 起订

￥663 5mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 AEE788

英文名称：: AEE788

CAS号：: 497839-62-0

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 98.94%

产品类别：: 抑制剂

货号：: T2116

Product Introduction

Bioactivity

名称	AEE788
描述	AEE788 (NVP-AEE 788) has been used in trials studying the treatment of Cancer, Glioblastoma Multiforme, and Brain and Central Nervous System Tumors.
细胞实验	Methylene Blue Cell Proliferation Assay.Cells are seeded at 1.5 × 103 cells/well into 96-well microtiter plates and incubated overnight at 37 °C, 5% v/v CO2 and 80% relative humidity. AEE788 dilutions are added on day 1, with the highest concentration being 10 μM. After incubation of the cell plates for an additional 4 (T24) or 6 (BT-474, SK-BR-3, and NCI-H596) days, cells are fixed with 3.3% v/v glutaraldehyde, washed with water, and stained with 0.05% w/v methylene blue. After washing, the dye is eluted with 3% HCl and the absorbance measured at 665 nm with a SpectraMax 340 spectrophotometer. IC50 values are determined by mathematical curve-fitting and are defined as the drug concentration leading to 50% inhibition of net cell mass increase compared with untreated control cultures. (Only for Reference)
激酶实验	Protein Kinase Assays: The in vitro kinase assays are performed in 96-well plates (30 μL) at ambient temperature for 15–45 min using the recombinant glutathione S-transferase-fused kinase domains (4-100 ng, depending on specific activity). [γ33P]ATP is used as phosphate donor and polyGluTyr-(4:1) peptide as acceptor. With the exception of protein kinase C-α, cyclin-dependent kinase 1/cycB and protein kinase A are protamine sulfate (200 μg/mL), histone H1 (100 μg/mL), and the heptapeptide Leu-Arg-Arg-Ala-Ser-Leu-Gly (known as Kemptide Bachem) respectively and are used as peptide substrates. Assays are optimized for each kinase using the following ATP concentrations: 1.0 μM (c-Kit, c-Met, c-Fms, c-Raf-1, and RET), 2.0 μM (EGFR, erbB2, ErbB3, and ErbB4), 5.0 μM (c-abl), 8.0 μM (Flt-1, Flt-3, Flt-4, Flk, KDR, FGFR-1, and Tek), 10.0 μM (PDGFR-β, protein kinase C-α, and cyclin-dependent kinase 1), and 20.0 μM (c-Src and protein kinase A). The reaction is terminated by the addition of 20 μL 125 mM EDTA. Thirty μL (c-abl, c-Src, insulin-like growth factor-1R, RET-Men2A, and RET-Men2B) or 40 μL (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 200 μL 0.5% H3PO4. Membranes are removed and washed four times with 1.0% H3PO4 and once with ethanol. Dried membranes are counted after mounting in a Packard TopCount 96-well frame and with the addition of 10 μL/well of Microscint. IC50 values (±SE) are calculated by linear regression analysis of the percentage inhibition and are averages of at least three determinations.
体外活性	AEE788（50 mg/kg）抑制盲肠和腹膜肿瘤的生长（> 50％）,并将植入裸鼠盲肠的HT29细胞的淋巴结转移发生率降低至70％,对体重无影响.50 mg/kg AEE788作用于NeuT/ErbB2 GeMag模型诱导肿瘤消退达57%.AEE788有效抑制A431肿瘤中的EGF诱导的EGFR磷酸化和GeMag肿瘤中的erbB2磷酸化.AEE788在NCI-H596或DU145异种移植模型中产生对肿瘤生长的剂量依赖性抑制,仅有轻微的体重变化.AEE788作用于K562肿瘤细胞,可以促进LBH589调节的活性氧簇的产生,可以增强凋亡. AEE788剂量依赖性地抑制由VEGF诱导的血管生成并且不抑制bFGF诱导的血管生成.AEE788作用于HT29盲肠癌,明显降低pEGFR和pVEGFR 的表达水平,但是不改变EGF,VEGF,EGFR或VEGFR的表达水平.和CPT-11联用,AEE788明显抑制淋巴癌转移 AEE788抑制Daoy,DaoyPt和DaoyHER2移植瘤的生长,抑制分别达51%,45%和72%.
体内活性	0.2-1.0 μM AEE788抑制HT29细胞中EGFR和Akt的磷酸化。AEE788抑制人皮肤SCC细胞系（Colo16,HaCaT,SRB1和SRB12细胞）中EGFR,VEGFR2,Akt和MAPK的磷酸化,导致生长抑制和诱导细胞凋亡。 AEE788有效抑制A431细胞中的EGFR磷酸化,IC5??0为11 nM。 AEE788还抑制CHO细胞中KDR的磷酸化和BT-474细胞中的erbB2的磷酸化,而对A31细胞中的PDGF-诱导的磷酸化没有任何影响。AEE788作用于髓母细胞瘤细胞系,抑制细胞增殖,抑制EGF和神经调节蛋白诱导的HER1,HER2和HER3激活。AEE788抑制NCI-H596,MK,BT-474和SK-BR-3细胞增殖,IC50分别为78,56,49和381 nM。AEE788也抑制EGF和VEGF促进的人脐静脉内皮细胞增殖,IC50分别为43和155 nM。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 82 mg/mL (186.1 mM)
关键字	Apoptosis \| HER1 \| Inhibitor \| Epidermal growth factor receptor \| AEE788 \| NVP-AEE788 \| ErbB-1 \| inhibit \| NVP-AEE-788 \| AEE-788 \| AEE 788 \| EGFR
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NVP-AEE 788|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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