MK-2461
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.
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
