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 Details
| Alternative Name: | AZD-6244, ARRY-142886 |
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| Formula: | C17H15BrClFN4O3 |
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| MW: | 457.7 |
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| CAS: | 606143-52-6 |
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| Purity: | ≥95% (HPLC) |
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| Identity: | Determined by EM-MS. |
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| Appearance: | Beige powder. |
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| Solubility: | Soluble in DMSO (92mg/ml) or ethanol (<1mg/ml). |
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| Shipping: | Ambient |
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| Short Term Storage: | +4°C |
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| Long Term Storage: | -20°C |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
Effects of thiostrepton alone or in combination with selumetinib on triple-negative breast cancer metastasis: F.D. Korkmaz, et al.; Mol. Biol. Rep.
49, 10387 (2022),
Abstract;
