AMG-208
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-208是一种高选择性的c-Met抑制剂，IC50值为9.3 nM[1]。c-Met是一种受体酪氨酸激酶，其天然配体是肝细胞生长因子（HGFa），对于正常胚胎发育是必需的，参与细胞增殖、迁移和侵袭[2]。
AMG-208是一种选择性的c-Met抑制剂。用AMG-208预孵育人肝微粒体30分钟，以时间依赖的方式抑制8倍的CYP3A4代谢活性，IC50值为4.1 μM[1]。在PC3细胞中，AMG-208抑制HGF介导的c-Met磷酸化，IC50值为46 nM [2]。
在雄性Sprague-Dawley大鼠中，静脉注射给药AMG-208 0.5 mg/kg，AMG-208呈现出高的生物利用度， Cl值为0.37 L/h/kg，药物几何平均分布容积（Vss）为0.380.38 L/kg，T1/2值为1小时[2]。c-Met失调与几种人类癌症相关，AMG-208可以抑制c-Met的活性，可用于癌症治疗[1]。
参考文献：
[1]. Boezio AA, Berry L, Albrecht BK, et al. Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors. Bioorg Med Chem Let,. 2009, 19(22): 6307-6312.
[2]. Albrecht BK, Harmange JC, Bauer D, et al. Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase. J Med Chem, 2008, 51(10): 2879-2882.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 383.4 |
| Cas No. | 1002304-34-8 |
| Formula | C22H17N5O2 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥3.83 mg/mL in DMSO |
| Chemical Name | 7-methoxy-4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline |
| SDF | Download SDF |
| Canonical SMILES | COC1=CC2=NC=CC(=C2C=C1)OCC3=NN=C4N3N=C(C=C4)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 | AMG-208 is a potent and highly selective inhibitor of Met with IC50 value of 9.3 nM. | |||||
| Targets | Met | |||||
| IC50 | 9.3 nM | |||||
化学结构
