Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CH7233163 是一种EGFR-tyrosine kinase 的非共价ATP 竞争性抑制剂,对有EGFR-Del19/T790M/C797S 的肿瘤具有抗肿瘤活性。
产品描述 | CH7233163 是一种EGFR-tyrosine kinase 的非共价ATP 竞争性抑制剂,对有EGFR-Del19/T790M/C797S 的肿瘤具有抗肿瘤活性。 |
靶点活性 | EGFR: |
体外活性 | CH7233163 shows potent antitumor activities against tumor with EGFR-Del19/T790M/C797S in vitro. CH7233163 potently inhibits the proliferation of Del19/T790M/C797S_NIH3T3 cells with IC50 of 20 nmol/L. CH7233163 potently and dose-dependently blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 can inhibit Del19/T790M/C797S signaling.[1] |
体内活性 | Pharmacodynamic study is performed using Del19/T790M/C797S_NIH3T3 xenografted tumors in mice. CH7233163 clearly inhibits EGFR phosphorylation after oral administration and potent tumor regression is observed. CH7233163 has potent therapeutic efficacy against tumors with EGFR-Del19/T790M/C797S in vivo.[1] |
细胞实验 | Cell lines: NIH3T3 cells (ATCC) Concentrations: 8 nM, 40 nM, 200 nM, 1000 nM Incubation Time: 0.5 h-24 h, 4-7 days Method: NIH3T3 cells (ATCC) are transduced with lentiviruses harboring genes encoding the EGFR-d746-750/T790M/C797S or EGFR-L858R/T790M/C797S mutant, generated from the pCDH-CMV-MCS-EF1-Puro vector. Cells stably expressing these mutants are subsequently selected in medium supplemented with puromycin. Cells are incubated in medium containing serial dilutions of CH7233163 in a 96-well culture plate or PrimeSurface96U plates at 37?C for 4 or 7 d. The number of living cells is then determined using CellTiter-Glo 9 Luminescent Cell Viability Assay. |
分子量 | N/A |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
CH7233163 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR CH 7233163 CH-7233163 Inhibitor inhibitor inhibit