Products & ReviewLife Sciences
AZD6244
MEK/ERK pathway inhibitor; Inhibits MEK1 and MEK2
AZD6244
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AZD6244 is a potent, highly selective inhibitor of the mitogen-activated protein kinases MEK1 (IC₅₀ = 14 nM) and MEK2 (Kd = 530 nM; Yeh et al.; Davis et al.). It is a tight-binding noncompetitive inhibitor that does not bind in the ATP binding pocket of MEK (Huynh et al.). It also shows micromolar binding to epidermal growth factor receptor (EGFR; Davis et al.).
CANCER RESEARCH
- Inhibits growth of several tumor cell lines but not normal fibroblast lines, and inhibits tumor growth in a colorectal xenograft tumor model (Yeh et al.).
- Inhibits proliferation and induces differentiation and apoptosis in multiple tumor cell lines and tumor xenograft models, especially those containing BRAF or RAS mutations (Davies et al.).
- Inhibits proliferation of breast cancer and non-small cell lung cancer cell lines, especially those containing RAF and RAS mutations, respectively (Garon et al.).
