Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Alectinib (RG-7853) 是一种有效的、选择性的、口服具有活力的、ATP 竞争性的 ALK 抑制剂,其 IC50=1.9 nM,Kd=2.4 nM,并且还抑制 ALK F1174L 和 ALK R1275Q,其 IC50分别为 1 nM 和 3.5 nM。它还有中枢神经系统渗透能力。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 293 | 现货 | ||
2 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 690 | 现货 | ||
10 mg | ¥ 872 | 现货 | ||
25 mg | ¥ 1,390 | 现货 | ||
50 mg | ¥ 1,990 | 现货 | ||
100 mg | ¥ 3,180 | 现货 | ||
200 mg | ¥ 5,120 | 现货 | ||
500 mg | ¥ 7,770 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 748 | 现货 |
产品描述 | Alectinib (RG-7853) is an orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity. |
靶点活性 | ALK:1.9 nM, ALK (R1275Q):3.5 nM, ALK (F1174L):1 nM |
体外活性 | 在小鼠中,CH5424802(20 mg/kg)处理能够抑制肿瘤生长.CH5424802 (2-20 mg/kg)以剂量依赖的方式抑制STAT3磷酸化. |
体内活性 | 在表达EML4-ALK的NCI-H2228NSCLC细胞中,CH5424802防止ALK自磷酸化。 在NCI-H2228球状体细胞中, CH5424802诱导凋亡标记 - 半胱天冬酶-3/7样活化。 在淋巴瘤细胞系KARPAS-299和SR与NPM-ALK中, CH5424802阻断融合蛋白的生长。CH5424802对天然ALK(Ki=0.83 nM)和L1196M(Ki=1.56 nM)都具有显着的抑制效力。 CH5424802抑制KAPRAS-299(IC50=3 nM),KDR(IC50=1.4 μM)。 |
激酶实验 | Kinase inhibitory assays in Vitro: The inhibitory ability against each kinase except for MEK1 and Raf-1 is evaluated by examining their ability to phosphorylate various substrate peptides in the presence of CH5424802 using time-resolved fluorescence resonance energy transfer (TR-FRET) assay or fluorescence polarization (FP) assay. The inhibitory activity against MEK1 is evaluated by quantitative analysis of the phosphorylation of a substrate peptide by a recombinant ERK2 protein in the presence of CH5424802. The inhibitory activity against Raf-1 is evaluated by examining the ability of the kinases to phosphorylate MEK1 in the presence of CH5424802. |
细胞实验 | Cells including NSCLC, A549 and HCC827 are seeded in 96-well plates overnight and incubated with various concentrations of CH5424802 for the indicated time. For spheroid cell growth inhibition assay, cells are seeded on spheroid plates, incubated overnight, and then treated with compound for the indicated times. The viable cells are measured by the Luminescent Cell Viability Assay. Caspase-3/7 assay is evaluated using the Caspase-Glo 3/7 Assay Kit.(Only for Reference) |
别名 | 阿来替尼, RG-7853, 艾乐替尼, AF802, CH5424802, AF-802 |
分子量 | 482.62 |
分子式 | C30H34N4O2 |
CAS No. | 1256580-46-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 2.1 mM
DMSO: 4.83 mg/mL (10 mM), Sonification is recommended
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 2.072 mL | 10.3601 mL | 20.7202 mL | 51.8006 mL |
DMSO | 5 mM | 0.4144 mL | 2.072 mL | 4.144 mL | 10.3601 mL |
10 mM | 0.2072 mL | 1.036 mL | 2.072 mL | 5.1801 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。
Alectinib 1256580-46-7 Angiogenesis Tyrosine Kinase/Adaptors VEGFR Tyrosine Kinases ALK ALK tyrosine kinase receptor RO-5424802 RO5424802 Anaplastic lymphoma kinase CD246 阿来替尼 RG-7853 RG 7853 inhibit RG7853 艾乐替尼 AF802 CH5424802 Inhibitor CH 5424802 AF 802 Cluster of differentiation 246 Anaplastic lymphoma kinase (ALK) AF-802 RO 5424802 CH-5424802 inhibitor