AdipoGen Selumetinib

Supplier:  AdipoGen AGCR13757M010

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 p38α, 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.

Catalog No. 50-256-2168