Selumetinib is a non-ATP competitive inhibitor of MEK-1 (IC50 = 14 nM). This compound inactivates the phosphorylation of ERK1/2 (IC50 < 40 nM). Selumetinib has little effect on p38, c-Jun-NH2-kinase, or the MEK/ERK5 pathways.
Crystalline granules or crystalline powder
Soluble in DMSO (92 mg/ml at 25 °C), water (<1 mg/ml at 25 °C), and ethanol (<1 mg/ml at 25 °C).
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DreadenDreaden, EC. et al. (PubMed 26034127) co-encapsulated AZD6244 (Selumetinib), an inhibitor of Mek1/2, and PX-866 (sc-396764), an inhibitor of PI3K, to create tumor-targeting nanoscale drug formulation-layer-by-layer (LbL) nanoparticles. Combined MAPK and PI3K axis blockade from the nanoscale formulations was synergistically toxic toward triple-negative breast (MDA-MB-231) and RAS-mutant lung tumor cells (KP7B) in vitro. -SCBT Publication Review
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