Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CNX-2006 是一种新型的不可逆突变选择性 EGFR 抑制剂,对 EGFRT790M 的IC50值小于 20 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 298 | 现货 | ||
2 mg | ¥ 438 | 现货 | ||
5 mg | ¥ 778 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,280 | 现货 | ||
50 mg | ¥ 3,320 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 946 | 现货 |
产品描述 | CNX-2006 is a novel irreversible mutant-selective EGFR inhibitor with IC50 of < 20 nM, with very weak inhibition at wild-type EGFR. |
靶点活性 | EGFR (mutant):<20 nM |
体外活性 | CNX-2006 is a novel irreversible EGFR tyrosine kinase inhibitor, specifically inhibits activating mutations of EGFR as well as the T790M mutation while having very weak inhibition at wild-type EGFR. In in vitro modeling of acquired resistance, continuous CNX-2006 treatment on drug-sensitive EGFR mutant cells leads to resistance more slowly than erlotinib. Dose escalation with CNX-2006 leads to differential effects in different lines, but does not select for T790M-mediated resistance. [1]CNX-2006 resistent cells shows increased expression of EMT markers and MMP9.[2] |
体内活性 | CNX-2006 is effective in H1975 (EGFR L858R/T790M) xenograft model. [1] [2] |
激酶实验 | Growth inhibition assays: Human EGFR mutant lung adenocarcinoma cell lines are treated with drugs in standard growth inhibition assays. |
细胞实验 | Cells with endogenous or transiently transfected mutant EGFRs (293 cells) are treated with inhibitors for 6 hours and then corresponding lysates are extracted and analyzed by immunoblotting.(Only for Reference) |
动物实验 | Animal Models: Nude miceFormulation: 5% DMSO:15% Solutol HS15 in PBSDosages: 25 mg/kgAdministration: i.p. |
别名 | CNX 2006, CNX2006 |
分子量 | 545.53 |
分子式 | C26H27F4N7O2 |
CAS No. | 1375465-09-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMF: soluble
DMSO: 91 mg/mL(166.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.8331 mL | 9.1654 mL | 18.3308 mL | 45.827 mL |
5 mM | 0.3666 mL | 1.8331 mL | 3.6662 mL | 9.1654 mL | |
10 mM | 0.1833 mL | 0.9165 mL | 1.8331 mL | 4.5827 mL | |
20 mM | 0.0917 mL | 0.4583 mL | 0.9165 mL | 2.2913 mL | |
50 mM | 0.0367 mL | 0.1833 mL | 0.3666 mL | 0.9165 mL | |
100 mM | 0.0183 mL | 0.0917 mL | 0.1833 mL | 0.4583 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。
CNX-2006 1375465-09-0 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR CNX 2006 HER1 inhibit Epidermal growth factor receptor ErbB-1 CNX2006 Inhibitor inhibitor