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Selumetinib

Chemical Structure : Selumetinib

CAS No.: 606143-52-6

Selumetinib (ARRY-142886;AZD-6244)

Catalog No.: PC-45849Not For Human Use, Lab Use Only.

Selumetinib (ARRY-142886, AZD-6244) highly potent and selective, ATP-uncompetitive inhibitor of MEK1/2 with IC50/Ki of 14.1 nM/22.6 nM for MEK1.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Selumetinib (ARRY-142886, AZD-6244) highly potent and selective, ATP-uncompetitive inhibitor of MEK1/2 with IC50/Ki of 14.1 nM/22.6 nM for MEK1.
Selumetinib (ARRY-142886, AZD-6244) shows no activity against other 40 serine/threonine and tyrosine kinases.
Selumetinib (ARRY-142886, AZD-6244) inhibits cellular ERK1/2 phosphorylation (IC50<40 nM), suppresses growth inhibition of several cell lines containing B-Raf and Ras mutations (IC50=59-473 nM).
Selumetinib (ARRY-142886, AZD-6244) causes growth of HT-29 xenograft tumors in nude mice.

Physicochemical Properties

M.Wt 457.6814
Formula C17H15BrClFN4O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 34 mg/mL

Chemical Name/SMILES

1H-Benzimidazole-6-carboxamide, 5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-

References

1. Huynh H, et al. Mol Cancer Ther. 2007 Jan;6(1):138-46.

2. Yeh TC, et al. Clin Cancer Res. 2007 Mar 1;13(5):1576-83.

3. Davies BR, et al. Mol Cancer Ther. 2007 Aug;6(8):2209-19.

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