Binimetinib
MEK1/2 inhibitor / Binimetinib (606143-89-9) is a potent (IC50 = 12 nM) and selective allosteric inhibitor of MEK1/2.1,2 Recently approved by the FDA for treatment of melanoma in combination with Encorafenib. Binimetinib has had limited success as monotherapy but has shown promise in combination with other chemotherapeutic agents.3-5
Biochemicals & reagents
606143-89-9
ARRY-162; MEK162
1) Lee et al. (2010), Preclinical development of ARRY-162, a potent and selective MEK1/2 inhibitor; Cancer Res. 70 2515 2) Winski et al. (2010), MEK162 (ARRY-162), a novel MEK ½ inhibitor, inhibits tumor growth regardless of KRAS/RAF pathway mutations; EJC Supplements 8 56 3) Lee et al. (2016), Efficacy of the combination of MEK and CDK4/6 inhibitors in vitro and in vivo in KRAS mutant colorectal cancer models; Oncotarget 7 39595 4) Gong et al. (2017), MEK162 Enhances Antitumor Activity of 5-Fluorouracil and Trifluridine in KRAS-mutated Human Colorectal Cancer Cell Lines; Anticancer Res. 37 2831 5) Van Cutsem et al. (2019), Binimetinib, Encorafenib, and Cetuximab Triplet Therapy for Patients With BRAF V600E-Mutant Metastatic Colorectal Cancer: Safety Lead-In Results From Phase III BEACON Colorectal Cancer study; J. Clin. Oncol. 180 2459
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TARGET: Kinase -- PATHWAY: Proliferation; PI3K; ERK -- DISEASE AREA: Cancer