Selumetinib

Product description: Chemical. CAS: 606143-52-6. Formula: C17H15BrClFN4O3. MW: 457.7. Selumetinib is an orally available, potent and selective ATP non-competitive inhibitor of the mitogen-activated protein kinases MEK1 (IC50 = 14 nM) and MEK2 (Kd = 530 nM). MEK1 and MEK2 specifically act downstream of growth factor receptors and the proto-oncogenes Ras and Raf to activate ERK1 and ERK2, often leading to an increase in cell proliferation. It inhibits ERK1/2 phosphorylation (IC50 = 10 nM), but exhibits only weak activity at p38?, MKK6, EGFR, ErbB2 and ERK2. Selumetinib inhibits growth of several tumor cell lines but not normal fibroblast lines and shows potent dose-dependent antitumor activity against a panel of mouse xenograft models of colorectal, pancreatic, liver, skin and lung cancer. It inhibits proliferation and induces differentiation and apoptosis in multiple tumor cell lines and tumor xenograft models, and inhibits proliferation of breast cancer and non-small cell lung cancer cell lines, especially those containing Raf and Ras mutations, respectively.

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