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Submit ReviewSelumetinib
说明： Potent and selective MEK inhibitor; orally bioavailable
化学名： 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide
纯度： ≥98% (HPLC)
生物活性 for Selumetinib
Selumetinib is a potent and selective MEK inhibitor (IC50 = 14 nM for MEK1, Kd = 530 nM for MEK2). Inhibits ERK1/2 phosphorylation (IC50 = 10 nM). Exhibits no activity at p38α, MKK6, EGFR, ErbB2 and ERK2. Suppresses several cell lines containing B-Raf and Ras mutations, but displays no effect on a normal fibroblast cell lines. Inhibits tumor growth in colorectal tumor xenograft model. Orally bioavailable.
技术数据 for Selumetinib
| 分子量 | 457.68 |
| 公式 | C17H15BrClFN4O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 606143-52-6 |
| PubChem ID | 10127622 |
| InChI Key | CYOHGALHFOKKQC-UHFFFAOYSA-N |
| Smiles | CN1C=NC2=C(C(NC3=C(C=C(C=C3)Br)Cl)=C(C(NOCCO)=O)C=C12)F |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
产品说明书 for Selumetinib
参考文献 for Selumetinib
参考文献是支持产品生物活性的出版物。
Yeh et al (2007) Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin.Cancer Res. 13 1576 PMID: 17332304
Garon et al (2010) Identification of common predictive markers of in vitro response to the Mek inhibitor selumetinib (AZD6244; ARRY-142886) in human breast cancer and non-small cell lung cancer cell lines. Mol.Cancer Ther. 9 1985 PMID: 20587667
Huynh et al (2007) Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma. Mol.Cancer Ther. 6 138 PMID: 17237274
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关键词: Selumetinib, Selumetinib supplier, Potent, selective, MEK, inhibitors, inhibits, ERK1/2, orally, bioavailable, active, in, vivo, 6815, Tocris Bioscience
1 篇 Selumetinib 的引用文献
引用文献是使用了 Tocris 产品的出版物。 Selumetinib 的部分引用包括：
Jonathan A et al (2023) Deep genomic analysis of malignant peripheral nerve sheath tumor cell lines challenges current malignant peripheral nerve sheath tumor diagnosis. iScience 26 106096 PMID: 36818284
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for Selumetinib
