AMG 337
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.
在酶测定中,IC50<5 nM。
AMG 337是一种MET抑制剂。
MET受体及其配体可以促进细胞存活、增殖和侵袭。MET信号传导的激活是多种人类癌症类型的常见调节剂,因此,抑制MET信号传导是一种有希望的癌症治疗机会。
体外:AMG 337可以有效抑制MET激酶活性,并且针对超过400种蛋白质以及脂质激酶进行测试时,AMG 337也显示出对MET的高选择性。此外,研究发现AMG 337抑制HGF依赖性MET磷酸化。此外,AMG 337只能影响具有MET基因扩增的两种胃癌细胞系的存活力。AMG 337对两种敏感细胞系的IC50值小于50 nM,而在所有其它测试的细胞系中超过10 μM [1]。
体内:在动物研究中发现,AMG 337口服给药导致MET扩增胃癌异种移植模型中剂量依赖性的抗肿瘤效果,这与MET信号传导的PD调节非常一致[1]。
临床试验:1期临床研究目前正在研究实体瘤患者中AMG 337的安全性、耐受性和PK [2]。
参考文献:
[1] Paul E. Hughes, et al. AMG 337, a novel, potent and selective MET kinase inhibitor, has robust growth inhibitory activity in MET-dependent cancer models. Cancer Res October 1, 2014 74; 728
[2] https://clinicaltrials. gov/ct2/show/NCT01253707term=AMG+337&rank=1
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 463.46 |
Cas No. | 1173699-31-4 |
Formula | C23H22FN7O3 |
Solubility | ≥46.3 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | (R)-6-(1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one |
SDF | Download SDF |
Canonical SMILES | CN1N=CC(C2=CN3C([C@@H](C)N4C=CC(N=CC(OCCOC)=C5)=C5C4=O)=NN=C3C(F)=C2)=C1 |
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。 |
质量控制和MSDS
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