Powder: -20°C for 3 years | In solvent: -80°C for 1 year
VX-11e (TCS ERK 11e) 是可口服的ERK 高效选择性抑制剂,Ki 值小于 2 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 321 | 现货 | ||
5 mg | ¥ 717 | 现货 | ||
10 mg | ¥ 1,090 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 790 | 现货 |
产品描述 | VX-11e (TCS ERK 11e) is a potent, selective, and orally bioavailable ERK(Extracellular Signal-Regulated Kinase) inhibitor; antitumor agent. |
靶点活性 | ERK2:<2 nM(Ki) |
体外活性 | In HT29 cells, VX-11e potently inhibits cell proliferation with IC50 of 48 nM. [1] |
体内活性 | In both rats and mice, VX-11e shows good oral bioavailability. [1] In NSG mice bearing human melanoma RPDX tumors, VX-11e (50 mg/kg, p.o.) results in robust inhibition of pRSK, and inhibits tumor growth. When used in combination with BKM120, VX-11e results in significantly improved tumor growth inhibition. [2] |
激酶实验 | ERK Inhibition Assay: Compounds are assayed for the inhibition of ERK2 by a spectophotometric coupled-enzyme assay. In this assay, a fixed concentration of activated ERK2 (10 nM) is incubated with various concentrations of the compounds in DMSO (2.5%) for 10 min. at 30 °C in 0.1 M HEPES buffer, pH = 7.5, containing 10 mM MgCl2, 2.5 mM phosphoenolpyruvate, 200 μM NADH, 150 μg/mL pyruvate kinase, 50 μg/mL lactate dehydrogenase and 200 μM erktide peptide. The reaction is initiated by the addition of 65 μM ATP. The rate of decrease of absorbance at 340 nM is monitored. The IC50 is evaluated from the data as a function of inhibitor concentr |
细胞实验 | Cell proliferation is measured by 3H-thymidine incorporation. The cells are plated at a concentration of 10,000 cells/well in a 96-well plate using growth media, RPMI 1640 containing 10% FBS. Serially diluted compounds are added. The cells and compounds are incubated for 48 hours at 37°C incubator. After 48 hours, 0.4 μCi of 3H-thymidine is added to each wells for 8 hours and returned to the 37°C incubator. The cells are harvested using a Tomtec 96-well cell harvester and the CPM is determined using the Wallac 1205 BETAPLATE liquid scintillation counter. The IC50 is the 50% inhibition of contr(Only for Reference) |
别名 | Vertex-11e, VTX-11e, TCS ERK 11e |
分子量 | 500.35 |
分子式 | C24H20Cl2FN5O2 |
CAS No. | 896720-20-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (100 mM)
Ethanol: 12.5 mg/mL (25 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.9986 mL | 9.993 mL | 19.986 mL | 49.965 mL |
5 mM | 0.3997 mL | 1.9986 mL | 3.9972 mL | 9.993 mL | |
10 mM | 0.1999 mL | 0.9993 mL | 1.9986 mL | 4.9965 mL | |
20 mM | 0.0999 mL | 0.4997 mL | 0.9993 mL | 2.4983 mL | |
DMSO | 50 mM | 0.04 mL | 0.1999 mL | 0.3997 mL | 0.9993 mL |
100 mM | 0.02 mL | 0.0999 mL | 0.1999 mL | 0.4997 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。
VX-11e 896720-20-0 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic MAPK PI3K/Akt/mTOR signaling Stem Cells Tyrosine Kinase/Adaptors ERK GSK-3 FLT CDK Aurora Kinase Extracellular signal regulated kinases Inhibitor inhibit Vertex-11e VTX-11e TCS ERK 11e VX 11e VX11e inhibitor