Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ulixertinib (VRT752271) 是一种有效且可逆的 ERK1/ERK2 抑制剂,可抑制 ERK2 和下游蛋白 RSK 的磷酸化,对 ERK2 的IC50值小于 0.3 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 335 | 现货 | ||
2 mg | ¥ 477 | 现货 | ||
5 mg | ¥ 822 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,390 | 现货 | ||
50 mg | ¥ 3,990 | 现货 | ||
100 mg | ¥ 5,680 | 现货 | ||
200 mg | ¥ 7,930 | 现货 | ||
500 mg | 特惠询价 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 861 | 现货 |
产品描述 | Ulixertinib (VRT752271) (BVD-523, VRT752271) is an effective and reversible ERK1/ERK2 inhibitor. The IC50 of Ulixertinib is less than 0.3 nM for ERK2. |
靶点活性 | ERK2:<0.3 nM |
体外活性 | In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM. [1] |
激酶实验 | ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay: MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 μL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 μM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 μL of substrate solution is added consisting of 16 μM Erktide (IPTTPITTTYFFFK) and 120 μM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 μl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels. |
细胞实验 | A375 cells are cultured in cell media composed of DMEM, 10% (v/v) Foetal Calf Serum and 1% (v/v) L-Glutamine. After harvesting, cells are dispensed into black, 384-well Costar plates to give 200 cells per well in a total volume of 40 μL cell media, and are incubated overnight at 37°C, 90% relative humidity and 5% CO2 in a rotating incubator. Test compounds and reference controls are dosed directly into the cell plates, into the inner 308 wells, using a Labcyte Echo 555 acoustic dispenser. The cells are dosed over a 12 point range from 30 μM down to 0.03 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 0.3%. The cell plates are then incubated for 72 hours at 37°C. Cells were fixed and stained by the addition of 20 μL 12% formaldehyde in PBS/A (4% final concentration) and 1:2000 dilution of Hoechst 33342, with a 30 minute room temperature incubation, and then washed with PBS/A. A cell count is performed on the stained cell plates using a Cellomics ArrayScanTM VTI imaging platform. A Day 0 cell plate is also fixed, stained and read to generate a cell count baseline for determining compound cytotoxic effects as well as anti-proliferative effects.(Only for Reference) |
别名 | BVD-523, VRT752271, 优立替尼 |
分子量 | 433.33 |
分子式 | C21H22Cl2N4O2 |
CAS No. | 869886-67-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 80 mg/mL (184.6 mM)
Ethanol: 12 mg/mL (27.7 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.3077 mL | 11.5386 mL | 23.0771 mL | 57.6928 mL |
5 mM | 0.4615 mL | 2.3077 mL | 4.6154 mL | 11.5386 mL | |
10 mM | 0.2308 mL | 1.1539 mL | 2.3077 mL | 5.7693 mL | |
20 mM | 0.1154 mL | 0.5769 mL | 1.1539 mL | 2.8846 mL | |
DMSO | 50 mM | 0.0462 mL | 0.2308 mL | 0.4615 mL | 1.1539 mL |
100 mM | 0.0231 mL | 0.1154 mL | 0.2308 mL | 0.5769 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。
Ulixertinib 869886-67-9 MAPK ERK VRT 752271 inhibit BVD 523 BVD-523 VRT-752271 BVD523 Inhibitor VRT752271 Extracellular signal regulated kinases 优立替尼 inhibitor