AMG-458
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AMG-458是人和小鼠c-Met的有效选择性抑制剂,IC50值分别是1.2 nM和2.0 nM。
c-Met又称为肝细胞生长因子受体,是由肝细胞生长因子/分散因子(HGF/SF)激活的受体酪氨酸激酶。它是一种膜蛋白,在胚胎发育和伤口愈合中起重要作用。
最近的研究表明,AMG-456对细胞放射增敏反应具有一定影响。结果表明,在c-Met表达较高的H441细胞中,AMG-458增强辐射敏感性,但对c-Met表达较低的A549没有作用[1]。
该物质被应用在动物模型中来研究c-Met在肿瘤发展中的作用。例如,在TPR-Met和U-87 MG肿瘤异种移植模型中,口服给药AMG-456,显著抑制肿瘤生长,但对体重没有任何不利的影响[2]。
参考文献:
1. Li B, Torossian A, Sun Y, Du R, Dicker AP, Lu B. Higher levels of c-Met expression and phosphorylation identify cell lines with increased sensitivity to AMG-458, a novel selective c-Met inhibitor with radiosensitizing effects. Int J Radiat Oncol Biol Phys 2012,84:e525-531.
2. Liu L, Siegmund A, Xi N, Kaplan-Lefko P, Rex K, Chen A, et al. Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-meth yl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). J Med Chem 2008,51:3688-3691.
Storage | Store at -20°C |
M.Wt | 539.58 |
Cas No. | 913376-83-7 |
Formula | C30H29N5O5 |
Synonyms | AMG 458; AMG458 |
Solubility | Soluble in DMSO |
Chemical Name | 1-(2-hydroxy-2-methylpropyl)-N-[5-(7-methoxyquinolin-4-yl)oxypyridin-2-yl]-5-methyl-3-oxo-2-phenylpyrazole-4-carboxamide |
SDF | Download SDF |
Canonical SMILES | CC1=C(C(=O)N(N1CC(C)(C)O)C2=CC=CC=C2)C(=O)NC3=NC=C(C=C3)OC4=C5C=CC(=CC5=NC=C4)OC |
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 | AMG 458是c-Met的有效抑制剂,Ki值为1.2 nM。 | |||||
靶点 | c-Met (H1094R) | c-Met (V1092I) | c-Met (Human) | c-Met (Mouse) | c-Met (D1228H) | |
IC50 | 0.5 nM(Ki) | 1.1 nM(Ki) | 1.2 nM(Ki) | 2.0 nM(Ki) | 2.2 nM(Ki) |
化学结构
![AMG-458](http://www.apexbt.com//media/diy/images/struct/A8361.png)