Selumetinib

5mg

Cat. No.: 07-V75

$89.00

Selumetinib, also known as AZD6244, is a potent inhibitor of MAPK/ERK kinase 1/2. It is not competitive with ATP and inactivates the ERK1/2 phosphorylation. This is important because these kinases lie downstream to BFAF and RAGS genes. The effect of mutation in these genes is controlled by inhibiting the kinases downstream.

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TECHNICAL INFORMATION

Other Names: 5-[(-bromo-2-chlorophenyl)amino]-4-fluoro-Nl-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide

Chemical Formula: C17H15CIFN4O3

CAS Number: 606143-52-6

Molecular Weight: 457.68

Purity: >99%

IC50= 14 nM

Appearance: Crystalline Solid

Solubility: DMSO (92mM)

 

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light. Following reconstitution, store  aliquots at -20°C. 

Stability: Stock solutions stable at -20°C for up to 2 years.

Shipping Conditions: Shipped at room temperature.

 

PRODUCT USE

Soluble in DMSO. Soluble at 92mg/ml

References

MS | B.B. | et al. (2012). Activity of the Mek inhibitor Selumetinib (AZD6244; ARRY-142886) in nasopharyngeal cancer cell lines. Invest New Drugs. S10637-012-9828-4.

Patel | S.P. | et al (2012). Selumetinib (AZD6244; ARRY-142886) in the treatment of metastatic melanoma. Expert Opin Investig Drugs. 21:531-9.

Holt | S.V. | et al (2012). The Mek 1/2 inhibitor | Selumetinib (AZD6244; ARRY-142886) | enhances anti-tumor efficacy when combined with conventional chemotherapeutic agents in human tumor xenograft models. Br J Cancer. 106:858-66.

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