Mirdametinib (PD0325901)

Description: Mirdametinib (PD-0325901) is a novel, potent, selective, orally bioavailable and non ATP-competitive inhibitor of the mitogen-activated protein kinase MEK with IC50 of 0.33 nM in cell-free assays, roughly 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. PD325901 is a derivative of MEK inhibitor CI-1040 that selectively binds to and inhibits MEK, which may result in the inhibition of the phosphorylation and activation of MAPK/ERK and the inhibition of tumor cell proliferation. MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors.

References: Mol Cancer Ther. 2010 Jul; 9(7):1968-76.