化合物Binimetinib T2508
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
100 mg | 606143-89-9 | ¥2,390.00 | 询底价 |
500 mg | 606143-89-9 | ¥5,950.00 | 询底价 |
1 mg | 606143-89-9 | ¥163.00 | 询底价 |
200 mg | 606143-89-9 | ¥3,820.00 | 询底价 |
25 mg | 606143-89-9 | ¥993.00 | 询底价 |
5 mg | 606143-89-9 | ¥356.00 | 询底价 |
10 mg | 606143-89-9 | ¥572.00 | 询底价 |
50 mg | 606143-89-9 | ¥1,580.00 | 询底价 |
1 mL | 606143-89-9 | ¥398.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Binimetinib
描述: Binimetinib (ARRY-162) 是一种可口服的选择性 MEK1/2抑制剂,抑制MEK 的IC50为 12 nM。
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].
体外活性: 在大鼠胶原诱导性关节炎模型中,ARRY-438162(1/3 mg/kg,2次/天,p.o.)抑制踝关节直径增加(27%/50%),而布洛芬处理可抑制46%.在大鼠佐剂诱发性关节炎模型中,ARRY-438162(3/10 mg/kg)抑制AIA踝关节直径(11%/34%).在注射MCF7-RSK4细胞的免疫缺陷小鼠,ARRY-438162(6 mg/kg,2次/天)与BEZ235联用可使肿瘤生长显著降低.在大鼠佐剂诱发性关节炎模型中,与对照组相比,ARRY-438162(10 mg/kg)剂量依赖地完全抑制血清中IL-6浓度.处理在大鼠胶原诱导性关节炎和佐剂诱发性关节炎模型中,ARRY-438162(10 mg/kg,2次/天p.o.)剂量依赖性地使疾病的严重程度降低.同样剂量处理大鼠胶原诱导性关节炎模型,可显著抑制病变(炎症,软骨损伤,血管翳形成,和骨重吸收), ARRY-438162(1/3 mg/kg)处理则分别抑制32%和60%.处理在大鼠佐剂诱发性关节炎模型中,与对照组相比,ARRY-438162(10/30 mg/kg)剂量依赖性地显著抑制踝关节肿胀.
体内活性: ARRY-438162是ATP非竞争性的MEK1/2抑制剂,可抑制细胞内pERK(IC50:11 nM)。MEK162(1 μM)与MK-2206(2 μM)联用可完全逆转表达RSK的MCF7细胞的抗性。ARRY-438162(2 μM)对成骨细胞分化的影响微弱。 ARRY-438162(10 μM)抑制体外破骨细胞再吸收(IC50:625 nM)。ARRY-438162(625 nM)抑制体外破骨细胞分化(IC50:39 nM)。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 50 mg/mL (113.32 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字: Inhibitor | MEK-162 | Mitogen-activated protein kinase kinase | MEK 162 | ARRY 162 | ARRY162 | ARRY438162 | MAPKK | MAP2K | Binimetinib | ARRY 438162 | inhibit | Autophagy | MEK
相关产品: GDC-0623 | Hederacolchiside A1 | trans-Zeatin | MS432 | RO4987655 | Corylifol C | zapnometinib | ZM-447439 | Isorhamnetin | MEK-IN-1
相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Approved Drug Library | Anti-Cancer Active Compound Library | EMA Approved Drug Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途