Selumetinib

Product Description

Selumetinib is a potent and selective MEK inhibitor (IC₅₀ = 14 nM for MEK1, K_d = 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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

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

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Garon 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. 2010 PMID: 20587667
• Huynh Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma. Mol.Cancer Ther. 2007 PMID: 17237274
• Yeh Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin.Cancer Res. 2007 PMID: 17332304