MK-2461
![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.
MK-2461是Met、Flt1、Flt3、Ron、PDGFRβ和Mer的高效抑制剂,IC50值分别为2.5 nM、10 nM、22 nM、7 nM和24 nM。
c-Met也称为肝细胞生长因子受体(HGFR),是一种受体酪氨酸激酶,在胚胎发育和伤口愈合中起重要作用。c-Met在多种肿瘤细胞中过表达或突变,在肿瘤细胞增殖、生存、侵袭、转移和血管形成中发挥重要作用。
体外实验:MK-2461处理能抑制肝细胞生长因子/c-Met依赖的有丝分裂、迁移、细胞离散和小管生成[1]。
体内试验:小鼠c-Met依赖的胃癌异体移植模型中,按100 mg/kg一天两次口服MK-2461能够有效抑制c-Met信号通路和肿瘤生长[1]。同样的,MK-2461也抑制皮下注射表达致癌c-Met突变的小鼠NIH-3T3细胞而形成的肿瘤的生长。这些证据支持MK-2461用于癌症治疗的临床前开发。
参考文献:
Pan BS, Chan GK, Chenard M, et al. MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer research. 2010;70(4):1524-1533.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 495.55 |
Cas No. | 917879-39-1 |
Formula | C24H25N5O5S |
Solubility | ≥24.8 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH |
Chemical Name | 9-[[[(2R)-1,4-dioxan-2-yl]methyl-methylsulfamoyl]amino]-2-(1-methylpyrazol-4-yl)-11-oxobenzo[1,2]cyclohepta[2,4-b]pyridine |
SDF | Download SDF |
Canonical SMILES | CN1C=C(C=N1)C2=CN=C3C=CC4=C(C=C(C=C4)NS(=O)(=O)N(C)CC5COCCO5)C(=O)C3=C2 |
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 | MK-2461是C-Met(野生型/突变型)高效多靶点抑制剂,其IC50值为0.4-2.5 nM。 | |||||
靶点 | c-Met (M1250T) | c-Met (Y1235D) | c-Met (Y1230H) | c-Met (N1100) | c-Met (Y1230C | c-Met |
IC50 | 0.4 nM | 0.5 nM | 1.0 nM | 1.5 nM | 1.5 nM | 2.5 nM |
化学结构
![MK-2461](http://www.apexbt.com//media/diy/images/struct/A8476.png)