AEE788 (NVP-AEE788)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AEE788是EGFR和HER2的有效抑制剂,IC50值分别为2 nM和6 nM。
表皮生长因子受体(EGFR)是一种细胞表面受体酪氨酸激酶。受体活化导致二聚化和酪氨酸自磷酸化。它诱导一系列下游细胞应答级联反应,如基因表达修饰、细胞增殖和细胞骨架重排等。
在HCT 15结肠癌细胞中,AEE788增强塞来昔布(celecoxib)介导的增殖和血管生成的阻断[1]。在EGFR和HER2过表达的各种细胞系中,AEE788表现出抗增殖活性[3]。AEE788还抑制细胞增殖,IC50 为1.7-3.8 μM,抑制表皮生长因子和体外神经调节蛋白诱导的HER1、HER2和HER3的活化[5]。
与对照小鼠相比,AEE788治疗21天后,抑制54%的肿瘤生长[2]。在ZR75.1 A3异种移植小鼠中,与单独来曲唑治疗相比,来曲唑与AEE788结合使用显著抑制肿瘤生长[4]。
参考文献:
[1] Venkatesan P, Bhutia SK, Singh AK et al. AEE788 potentiates celecoxib-induced growth inhibition and apoptosis in human colon cancer cells. Life Sci. 2012 Oct 22;91(15-16):789-99.
[2] Park YW, Younes MN, Jasser SA et al. AEE788, a dual tyrosine kinase receptor inhibitor, induces endothelial cell apoptosis in human cutaneous squamous cell carcinoma xenografts in nude mice. Clin Cancer Res. 2005 Mar 1;11(5):1963-73.
[3] Traxler P, Allegrini PR, Brandt R et al. 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. 2004 Jul 15;64(14):4931-41.
[4] Evans AH, Pancholi S, Farmer I et al. EGFR/HER2 inhibitor AEE788 increases ER-mediated transcription in HER2/ER-positive breast cancer cells but functions synergistically with endocrine therapy. Br J Cancer. 2010 Apr 13;102(8):1235-43.
[5] Meco D, Servidei T, Zannoni GF et al. Dual Inhibitor AEE788 Reduces Tumor Growth in Preclinical Models of Medulloblastoma. Transl Oncol. 2010 Oct 1;3(5):326-35.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 440.58 |
Cas No. | 497839-62-0 |
Formula | C27H32N6 |
Solubility | ≥22.05 mg/mL in DMSO; insoluble in H2O; ≥14.4 mg/mL in EtOH with ultrasonic |
Chemical Name | 6-[4-[(4-ethylpiperazin-1-yl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine |
SDF | Download SDF |
Canonical SMILES | CCN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(N3)N=CN=C4NC(C)C5=CC=CC=C5 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | AEE788(NVP-AEE788)是EGFR和HER2/ErbB2的有效抑制剂,IC50值分别为2 nM和6 nM。 | |||||
靶点 | EGFR | HER2/ErbB2 | c-Abl | FLT1 | c-Fms | |
IC50 | 2 nM | 6 nM | 52 nM | 59 nM | 60 nM |
质量控制和MSDS
- 批次: