产品描述:
PD 0325901 is a potent and selective non-ATP competitive orally active MEK1 and MEK2 inhibitor. In comparison to the CI-1040 MEK inhibitor, PD 0325901 has a greater potency of inhibition, longer duration, greater solubility, improved bioavailability and increased metabolic stability. The dual specific threonine/tyrosine kinase MEK is a key component of the RAS/RAF/MEK/ERK signaling pathway that is frequently activated in human tumors. This cell permeable inhibitor of the MEK/ERK pathway inhibits the activation and downstream signaling of MEK. PD 0325901 is an anti-cancer agent that is highly effective at inhibiting cell growth and proliferation in various cancer cells. It has been shown to inhibit MEK activity and suppresses phosphorylation of ERK in mouse colon 26 cells (IC50 = 0.33nM) and the growth of melanoma cell lines in vitro and in vivo. It induces G1-phase cell cycle arrest and apoptosis in a mouse xenograft model and inhibits production of proangiogenic cytokines such as VEGF. This derivative of MEK inhibitor CI-1040 is 500-fold more potent than CI-1040 on phosphorylation of ERK1 and ERK2. PD 0325901 promotes reprogramming of human somatic cells to iPSCs and enhances generation and self-renewal of induced pluripotent stem cells (iPSCs) in combination with other compounds.