Selumetinib

Product description: Selumetinib (AZD6244) is a second-generation, orally available, potent and selective ATP non-competitive inhibitor of MEK 1/2. In direct assays, AZD6244 selectively inhibits purified active MEK1 and MEK2 with an IC(50) of 14nM, and AZD6244 has reported IC(50) values of <100nm for MEK1 in ELISA assays and in bindings assays against recombinant domains of MEK2, Kd values were 53nM for AZD6244. AZD6244 demonstrated very effective anti-proliferation effects against several different cell lines with IC(50) values ranging from a low of 3nM to < 1µM depending upon the cell system used, and the compound inhibits basal and growth factor-stimulated phosphorylation of ERK1/ 2 with IC(50) concentrations < 40nM. AZD6244 has demonstrated potent dose-dependent antitumor activity against a panel of mouse xenograft models of colorectal, pancreatic, liver, skin, and lung cancer, and inhibition of tumor growth was found to correlate with the reduction of phospho-ERK1/2 levels in tumors.

Alternate Names/Synonyms: AZD6244; ARRY-142886

Product Type: Chemical

Molecular Formula: C17H15BrClFN4O3

Molecular Weight: 457.7

CAS: 606143-52-6

Purity: >95%

InChiKey: CYOHGALHFOKKQC-UHFFFAOYSA-N

Appearance Solid.

Solubility: Soluble in DMSO. Slightly soluble (<1mg/ml) in ethanol.

Short Term Storage: +4°C

Long Term Storage: -20°C

Shipping: AMBIENT

Use & Stability: Stable for at least 2 years after receipt when stored at -20°C.

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