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Submit ReviewSelumetinib
Description: Potent and selective MEK inhibitor; orally bioavailable
Chemical Name: 5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide
Purity: ≥98% (HPLC)
Biological Activity 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.
Technical Data for Selumetinib
| M. Wt | 457.68 |
| Formula | C17H15BrClFN4O3 |
| Storage | Store at -20°C |
| Purity | ≥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 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Selumetinib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 9.15 | 20 |
Preparing Stock Solutions for Selumetinib
The following data is based on the product molecular weight 457.68. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 10.92 mL | 54.62 mL | 109.25 mL |
| 1 mM | 2.18 mL | 10.92 mL | 21.85 mL |
| 2 mM | 1.09 mL | 5.46 mL | 10.92 mL |
| 10 mM | 0.22 mL | 1.09 mL | 2.18 mL |
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Product Datasheets for Selumetinib
References for Selumetinib
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for Selumetinib, please let us know.
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Keywords: Selumetinib, Selumetinib supplier, Potent, selective, MEK, inhibitors, inhibits, ERK1/2, orally, bioavailable, active, in, vivo, 6815, Tocris Bioscience
Citations for Selumetinib
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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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
