Powder: -20°C for 3 years | In solvent: -80°C for 1 year
RO4987655 (RG7167) 是一种具有口服活性和高选择性的 MEK 抑制剂,抑制MEK1/MEK2,IC50为 5.2 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 427 | 现货 | ||
2 mg | ¥ 619 | 现货 | ||
5 mg | ¥ 993 | 现货 | ||
10 mg | ¥ 1,650 | 现货 | ||
25 mg | ¥ 2,650 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,230 | 现货 |
产品描述 | RO4987655 (RG7167) is an orally active and highly selective MEK inhibitor (IC50: 5.2 nM for MEK1/MEK2). |
靶点活性 | MEK2:5.2 nM (cell free), MEK1:5.2 nM (cell free) |
体外活性 | CH4987655 (RO4987655) potently inhibits mitogen-activated protein kinase signaling pathway activation and tumor cell growth, with an in vitro IC50 of 5.2 nmol/L for inhibition of MEK1/2 [1]. In NCI-H2122 cells, RO4987655 at doses ranging from 0.1 to 1.0 μM suppressed pERK1/2 already at 2 h after the start of treatment. RO4987655 inhibited proliferation of NCI-H2122 cells in a dose-dependent manner with an IC50 value of 0.0065 μM [2]. |
体内活性 | In the dose-ranging study, treatment with RO4987655 5.0 mg/kg led to dramatic decrease in FDG uptake on day 1. The daily RO4987655, 2.5 mg/kg treatment were followed by PET examinations on days 1, 3, and 9 of the drug administration. The maximum decrease was observed on day 1, followed by a slight rebound on day 3. The effect plateaued thereafter to day 9 of treatment [2]. Doses of 0.5, 1, 2, 3, and 4 mg were safe and well-tolerated. A total of 26 adverse events (n = 15) were reported: 21 mild, 5 moderate, and none severe. Moderate adverse events were experienced by one subject at 1 mg (autonomic nervous system imbalance) and three subjects at 4 mg (diarrhea, abdominal pain, autonomic nervous system, and acne) [3]. |
细胞实验 | Cells were treated with various concentrations of RO4987655 for 72 h in 96-well plates and viable cells were quantified with Cell Counting Kit-8. For Western blotting, cells were treated with RO4987655 for indicated periods and lysed with cell lysis buffer containing a protease inhibitor cocktail, phosphatase inhibitor cocktails 2 and 3, and 1 mM PMSF. For detection of protein bands, the following were used as primary antibodies: pEGFR, EGFR, pMKK4, MKK4, pAKT, AKT, pERK, ERK, pMEK1/2, MEK, Cyclin D1, and actin. All protein bands were visualized with secondary antibodies labeled with HRP and ECL system by using ImageQuant LAS 4000 [2]. |
动物实验 | A time interval of 20 to 24 h was used between daily RO4987655 administration and completion of PET imaging for each tumor-bearing mouse and for each PET imaging time point (day 0, 1, 3 and 9). Mice were fasted for 6 to 8 h prior to start of the imaging session. [18F] FDG (7 to 8 MBq per mouse, maximum volume of 200 μL) was administered to awake, warmed (37°C) mice by a bolus injection via the tail vein. Forty to sixty minutes after the tracer injection, the mice were administered with isoflurane, controlled by an E-Z anesthesia vaporizer. The mice were placed on a heated pad (37°C) on the camera bed, with most of the body volume in the field of view (7.68 cm). Emission data were collected for 20 min in list mode with a microPET Focus 120 scanner. Maximum standardized uptake values (SUVmax) of [18F] FDG uptake in the tumor were calculated and normalized to the administered activity (MBq/body weight, g). The drug effect on tumor metabolism was estimated as%SUVmax change to day 0 (baseline) [2]. |
别名 | CH4987655, RG7167 |
分子量 | 565.28 |
分子式 | C20H19F3IN3O5 |
CAS No. | 874101-00-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 35 mg/mL (61.92 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.769 mL | 8.8452 mL | 17.6903 mL | 44.2259 mL |
5 mM | 0.3538 mL | 1.769 mL | 3.5381 mL | 8.8452 mL | |
10 mM | 0.1769 mL | 0.8845 mL | 1.769 mL | 4.4226 mL | |
20 mM | 0.0885 mL | 0.4423 mL | 0.8845 mL | 2.2113 mL | |
50 mM | 0.0354 mL | 0.1769 mL | 0.3538 mL | 0.8845 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
RO4987655 874101-00-5 MAPK MEK RG 7167 CH 4987655 RO 4987655 MAPKK Mitogen-activated protein kinase kinase MAP2K RO-4987655 Inhibitor CH4987655 inhibit RG-7167 RG7167 CH-4987655 inhibitor