Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.
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K882 is an inhibitor of Src kinase.1 It binds to Src (Kd = 315 nM), decreases phosphorylation at the tyrosine in position 416 (Y416), a Src activation site, and increases phosphorylation at Y527, an inactivation site. K882 reduces the proliferation of wild-type NCI H358 non-small cell lung cancer cells and NCI H358 cells expressing a KRASG12C mutation (IC50s = 2.14 and 2.03 µM, respectively). It also inhibits migration and invasion of NCI H358 cells when used at concentrations of 2, 4, and 8 µM, induces cell cycle arrest in the G2/M phase at 1, 4, and 8 µM, and induces apoptosis at 4 and 8 µM. K882 (25, 50, and 100 mg/kg) reduces tumor volume in an NCI H358 mouse xenograft model.
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1. Identification of a novel Src inhibitor K882 derived from quinazoline-