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Binimetinib (ARRY-162) 是一种 MEK1/2 抑制剂 (IC50=12 nM),具有选择性和口服活性。Binimetinib 具有抗肿瘤活性,用于治疗无法切除或具有 BRAF V600E 或 V600K 突变的转移性黑色素瘤。
Binimetinib (ARRY-162) 是一种 MEK1/2 抑制剂 (IC50=12 nM),具有选择性和口服活性。Binimetinib 具有抗肿瘤活性,用于治疗无法切除或具有 BRAF V600E 或 V600K 突变的转移性黑色素瘤。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 163 | 现货 | |
5 mg | ¥ 356 | 现货 | |
10 mg | ¥ 572 | 现货 | |
25 mg | ¥ 993 | 现货 | |
50 mg | ¥ 1,580 | 现货 | |
100 mg | ¥ 2,390 | 现货 | |
200 mg | ¥ 3,820 | 现货 | |
500 mg | ¥ 5,950 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 398 | 现货 |
产品描述 | 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. |
靶点活性 | MEK:12 nM |
体外活性 | 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] |
体内活性 | 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] |
细胞实验 | 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]. |
别名 | ARRY-438162, ARRY-162, MEK162 |
分子量 | 441.23 |
分子式 | C17H15BrF2N4O3 |
CAS No. | 606143-89-9 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (113.32 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) | |||||||||||||||||||||||||||||||||||
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DMSO
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