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Description: Refametinib (formerly RDEA-119, BAY 86-9766) is an orally bioavailable, highly selective and non-ATP-competitive (allosteric) inhibitor of MEK1/2 with potential antitumor activity. It inhibits MEK1/2with IC50s of 19 nM and 47 nM, respectively. It exhibits excellent anti-proliferative activity in vitro against cancer cell lines harboring V600E BRAF mutant, with GI50 values ranging from 67nM to 89nM. Furthermore, Refametinib demonstrated high in vivo antitumor efficacy in the human melanoma A375 tumor xenograft model and caused obvious tumor growth regression.
References: Cancer Res. 2009 Sep 1; 69(17):6839-47; Int J Cancer. 2010 Dec 15; 127(12):2965-73.
Related CAS: 923032-38-6 (Refametinib R enantiomer)
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