Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Icotinib (Conmana) 是一种口服的基于喹唑啉的表皮生长因子受体 (EGFR) 抑制剂,IC50值为5 nM,具有潜在的抗肿瘤活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 658 | 现货 | ||
2 mg | ¥ 839 | 现货 | ||
5 mg | ¥ 1,160 | 现货 | ||
10 mg | ¥ 1,730 | 现货 | ||
25 mg | ¥ 3,180 | 现货 | ||
50 mg | ¥ 4,790 | 现货 | ||
100 mg | ¥ 6,680 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,270 | 现货 |
产品描述 | Icotinib (Conmana) is an orally available quinazoline-based inhibitor of epidermal growth factor receptor (EGFR), with potential antineoplastic activity. |
靶点活性 | EGFR:5 nM |
体外活性 | Icotinib inhibits EGFR activity in a dose-dependent manner, with an IC50 value of 5 nM and complete inhibition at 62.5 nM. Icotinib selectively solely inhibits the EGFR members including the wild type and mutants with inhibition efficacies of 61-99%. Icotinib blocks EGFR-mediated intracellular tyrosine phosphorylation in human epidermoid carcinoma A431 cells in a dose-dependent manner. Meanwhile, in our proliferation assay performed on A431, BGC-823, A549, H460, HCT8, KB and Bel-7402 cell lines, we found that the relative sensitivity of cell lines to Icotinib is A431 > BGC-823 > A549 > H460 > KB > HCT8 and Bel-7402. Icotinib exhibits a broad spectrum of antitumor activity and it is especially effective against tumors expressing higher levels of EGFR. [1] |
体内活性 | Icotinib shows an antitumor effect in different types of xenografts. Icotinib inhibits tumor growth at a rate of 51.5%, 31.0% and 67.4% in the A431, A549 and H460 xenografts at a dose of 120 mg/kg, respectively. [1] |
激酶实验 | Biochemical kinase assays: In the in vitro kinase assays, 2.4 ng/μL EGFR protein is mixed with 32 ng/μL Crk in 25 μL kinase reaction buffer containing 1 μM cold ATP and 1 μCi 32P-γ-ATP. The mix is incubated with Icotinib at 0, 0.5, 2.5, 12.5 or 62.5 nM on ice for 10 min followed by incubation at 30 °C for 20 min. After quenching with SDS sample buffer at 100 °C for 4 min, the protein mix is resolved by electrophoresis in a 10% SDS-PAGE gel. The dried gel is then exposed to the PhosphorImager to detect radioactivity. Quantification is performed by ImageQuant software. In this methodology the radioactive signal inversely correlates with kinase activity. |
细胞实验 | Cells (103 /well) are seeded into 96-well plates in RPMI-1640 medium containing 10% FBS and grown in a 5% CO2 incubator at 37 °C. After 24 h, cells are treated with Icotinib at 0, 0.78, 1.56, 3.125, 6.25, 12.5 or 25 μM for 96 h. Cell proliferation is calculated by subtracting the mean absorbance value on day 0 from the mean absorbance value on day 4.(Only for Reference) |
别名 | BPI-2009, 埃克替尼, BPI-2009H, Conmana |
分子量 | 391.42 |
分子式 | C22H21N3O4 |
CAS No. | 610798-31-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 72 mg/mL (183.9 mM)
Ethanol: 6 mg/mL(15.3 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.5548 mL | 12.774 mL | 25.548 mL | 63.87 mL |
5 mM | 0.511 mL | 2.5548 mL | 5.1096 mL | 12.774 mL | |
10 mM | 0.2555 mL | 1.2774 mL | 2.5548 mL | 6.387 mL | |
DMSO | 20 mM | 0.1277 mL | 0.6387 mL | 1.2774 mL | 3.1935 mL |
50 mM | 0.0511 mL | 0.2555 mL | 0.511 mL | 1.2774 mL | |
100 mM | 0.0255 mL | 0.1277 mL | 0.2555 mL | 0.6387 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。
Icotinib 610798-31-7 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Inhibitor BPI-2009 埃克替尼 ErbB-1 BPI-2009H HER1 inhibit BPI 2009 BPI2009 Epidermal growth factor receptor Conmana inhibitor