AMG-458
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.
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) |