Pricing Availability   Qty
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)
Literature (4)
Pathways (1)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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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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

Citations are publications that use Tocris products.

Currently there are no citations for Selumetinib. Do you know of a great paper that uses Selumetinib from Tocris? Please let us know.

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Literature in this Area

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Pathways for Selumetinib

MAPK Signaling Pathway

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.