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Selumetinib

Potent and selective ATP non-competitive inhibitor of MEK1/2
 
ENZ-CHM184-0050 50 mg 110.00 USD
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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<(sub>50 of 14 nM, and AZD6244 has reported IC50 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 IC50 values ranging from a low of 3nM to < 1 µM depending upon the cell system used, and the compound inhibits basal and growth factor-stimulated phosphorylation of ERK1/ 2 with IC50 concentrations < 40 nM. 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.

Product Specification

Alternative Name:AZD-6244, ARRY-142886
 
Formula:C17H15BrClFN4O3
 
MW:457.7
 
CAS:606143-52-6
 
Purity:≥95% (HPLC)
 
Identity:Determined by EM-MS, NMR
 
Appearance:Beige powder.
 
Solubility:Soluble in DMSO (92mg/ml) or ethanol (<1mg/ml).
 
Shipping:Ambient
 
Short Term Storage:+4°C
 
Long Term Storage:-20°C
 
ENZ-CHM184 structure
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ENZ-CHM184 structure

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