Binimetinib (ARRY-162) is a MEK1/2 inhibitor (IC50=12 nM) with selective and oral activity. Binimetinib has antitumor activity for the treatment of metastatic melanoma that cannot be resected or has a BRAF V600E or V600K mutation.

MEK:12 nM

方法：神经母细胞瘤细胞用 Binimetinib (0-2 µM) 处理 24-120 h，通过 MTT assay 检测细胞活力。
结果：CHP-212、SK-N-BE、SK-N-AS 和 SJ-NB-10 四种细胞系对 Binimetinib 敏感，在治疗 24-120 h 后达到 <50%的存活率，而五种细胞系则对该药物产生耐药性。[1]
方法：NSCLC 细胞 A549、H157 和 H522 用 Binimetinib (0.5-1 µM) 处理 48 h，通过 flow cytometry 检测细胞周期。
结果：在相对较低浓度范围内，例如 0.5 和 1 µM，Binimetinib 在三种敏感的 NSCLC 细胞系中诱导 G1 期阻滞。[2]

方法：为检测体内抗肿瘤活性，将 Binimetinib (5 mg/kg) 和 BMK120 (7.5 mg/kg) 灌胃给药给携带 A549 异种移植物的 athymic (nu/nu) 小鼠，每天一次，持续 21 天。
结果：单独使用测试剂量的 Binimetinib 和 BKM120 仅对 A549 异种移植物的生长有微弱的抑制作用，但 Binimetinib 与 BKM120 的组合显著抑制了 A549 异种移动物的生长。[2]

MEK162 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[2]. MCF7 cells infected as indicated are seeded in 12-well plates (2×104). After 24 hours, cells are treated with BEZ235 (100 or 200 nM), BKM120 (0.75 or 1 μM), GDC-0941 (1 μM), or MK2206 (2 μM) alone or in combination with MEK162 (1 μM), BI-D1870 (10 μM), or AZD6244 (1 μM), as indicated in text. Cell numbers are quantified by fixing cells with 4% glutaraldehyde or methanol, washing the cells twice in Water, and staining the cells with 0.1% crystal violet. The dye is subsequently extracted with 10% acetic acid, and its absorbance is determined (570 nm). Growth curves are performed in triplicate. Viability assays with CellTiter-Glo are performed by plating 2,000 cells in 96-well plates, adding the drug at 24 hours, and assaying 4 to 5 days after drug addition. Cell-cycle and hypodiploid apoptotic cells are quantified by flow cytometry. Briefly, cells are washed with PBS, fixed in cold 70% ethanol, and then stained with propidium iodide while being treated with RNase. Quantitative analysis of sub-G1 cells is carried out in a FACScalibur cytometer using Cell Quest software[2].