Refametinib
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.
Refametinib是一种选择性的和可口服的MEK1和MEK2变构抑制剂，IC50值分别为19 nM和47 nM[1]。
Refametinib是一种非ATP竞争性的MEK1/2抑制剂。在体外实验中，refametinib抑制MEK1和MEK2的活性，IC50值分别为19 nM和47 nM。X射线分析表明，refametinib与MEK的变构位点结合，不影响ATP的结合，但阻止底物ERK的结合，从而阻止ERK的磷酸化。在多种人类肿瘤细胞中，包括A375、Colo205、HT-29和MDA-MB-231，refametinib抑制MEK的EC50值介于2.5 nM到15.8 nM之间。此外，在含V600E BRAF突变的肿瘤细胞系中，refametinib抑制细胞生长，GI50值介于67 nM到89 nM之间。而且，在人黑色素瘤A375肿瘤异种移植模型中，refametinib引起明显的肿瘤生长延迟和回归。Refametinib在人Colo205肿瘤异种移植模型中也具有肿瘤生长抑制作用[1]。
参考文献：
[1] Iverson C, Larson G, Lai C, et al. RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer. Cancer research, 2009, 69(17): 6839-6847.
| Storage | Store at -20°C |
| M.Wt | 572.34 |
| Cas No. | 923032-37-5 |
| Formula | C19H20F3IN2O5S |
| Solubility | insoluble in H2O; ≥151.8 mg/mL in DMSO; ≥90.2 mg/mL in EtOH |
| Chemical Name | N-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide |
| SDF | Download SDF |
| Canonical SMILES | COC1=CC(=C(C(=C1NS(=O)(=O)C2(CC2)CC(CO)O)NC3=C(C=C(C=C3)I)F)F)F |
| 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。 |
| 描述 | Refametinib（RDEA119，Bay 86-9766）是一种有效的、高选择性的和非ATP竞争性的MEK1和MEK2抑制剂，IC50值分别为19 nM和47 nM。 | |||||
| 靶点 | MEK1 | MEK2 | ||||
| IC50 | 19 nM | 47 nM | ||||
质量控制和MSDS
- 批次:
化学结构
