Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pelitinib (EKB-569) 是一种可逆的EGFR 抑制剂,IC50值为38.5 nM。它也抑制Src、MEK/ERK 和 ErbB2,IC50值分别为282、800 和 1255 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 269 | 现货 | ||
5 mg | ¥ 611 | 现货 | ||
10 mg | ¥ 987 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,320 | 现货 | ||
100 mg | ¥ 4,920 | 现货 | ||
500 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 611 | 现货 |
产品描述 | Pelitinib (EKB-569) (EKB-569) is an effective irreversible EGFR inhibitor (IC50: 38.5 nM). |
靶点活性 | EGFR:38.5 nM |
体外活性 | 在达EGFR的A431异种移植模型中,Pelitinib(10 mg/kg,p.o.)可有效抑制EGFR磷酸化,1 h内抑制90%,24 h后抑制率>50%.小鼠气道上皮细胞重构模型,可被病毒感染诱导,具有延迟但永久性转变为杯状细胞化生的特点,Pelitinib(20 mg/kg/day)可完全阻断纤毛细胞的增加和Clara细胞的减少,从而从3个方面校正上皮细胞重构,并明显抑制杯状细胞的发生.Pelitinib(20 mg/kg/day)抑制APCMin/+小鼠体内87%的肿瘤发生,与2倍剂量EKI-785(40 mg/kg/day)的作用接近,与体内活性较高一致. Pelitinib对体内气道上皮细胞中EGFR信号有选择性抑制效果. |
体内活性 | Pelitinib(75-500 nM)可特异性抑制AKT和ERK1/2的活化,而对NF-κB通路无影响。在正常人角质细胞中,Pelitinib也可有效抑制TGF-α介导的EGFR活化(IC50:56 nM),抑制STAT3和ERK1/2的活化(IC50:60 nM和62 nM)。在A431和正常人角质细胞中,Pelitinib对EGF诱导的EGFR磷酸化有抑制作用(IC50:20-80 nM),还抑制STAT3的磷酸化(IC50:30-70 nM)。 Pelitinib对正常人角质细胞(IC50:61 nM),以及A431(IC50:125 nM)和MDA-468(IC50:260 nM)肿瘤细胞的增殖有明显抑制作用,但对MCF-7细胞活性较低(IC50:3.6 μM)。 |
激酶实验 | Autophosphorylation of EGFR in cells: For experiments using cells in culture, A431 cells are treated with various concentrations of Pelitinib for 2.75 hours before co-incubation with 100 ng/mL EGF for 0.25 hour. Cells are washed twice with cold phosphate-buffered saline (PBS) before adding to lysis buffer (10 mM Tris, pH 7.5, 5 mM ethylenediamine tetra-acetic acid (EDTA), 150 mM NaCl, 1% Triton X-100, 1% Sodium deoxycholate, 0.1 % SDS, 1 mM PMSF, 10 mg/mL pepstatin A, 10 mg/mL leupeptin, 20 KIU/mL aprotinin, 2 mM sodium orthovanadate, and 100 mM sodium fluoride) for 20 minutes on ice, before immunoprecipitation and SDS-PAGE-immunoblotting. For immunoprecipitation, cultured cells are placed in cold lysis buffer and immediately homogenized on ice with a polytron with several pulses. The homogenate is first centrifuged at 2500 rpm (20 minutes, 4 °C) and then again at 14,000 rpm in a microcentrifuge (10 minutes, 4 °C). Supernatants (1000 μg protein) are incubated for 2 hours at 4 °C with 15 mL of EGFR polyclonal antibody. After 2 hours, 50 μL of protein G plus/protein A agarose beads is added and incubated with constant rotation for 2 hours at 4 °C. After washing with lysis buffer, beads are boiled for 2 minutes in Laemmli sample buffer. Proteins are then resolved by SDS-PAGE, transferred to immobilon membrane and probed overnight with an anti-phosphotyrosine antibody conjugated with horseradish peroxidase (HRP). Membranes are developed using the ECL reagent. Total EGFR protein is determined by stripping membranes and re-probing with receptor-specific antibodies. Quantitation of bands is done by densitometry, using ImageQuant software with a Molecular Dynamics laser transmittance scanner. |
细胞实验 | Cells are seeded in 96-well dishes, and after 2 hours, Pelitinib is added and incubated for 5 days. After incubation, the medium is removed from each well and fresh medium (150 μL) + 1 mg/mL MTT solution (50 μL) is added. After incubation for 2 hours at 37 °C, the medium is replaced with 150 μL DMSO, and absorbance at 540 nm in each well is determined. The IC50 is calculated by linear regression of the data. (Only for Reference) |
别名 | 培利替尼, EKB-569, WAY-EKB 569 |
分子量 | 467.92 |
分子式 | C24H23ClFN5O2 |
CAS No. | 257933-82-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 11 mg/mL (23.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1371 mL | 10.6856 mL | 21.3712 mL | 53.4279 mL |
5 mM | 0.4274 mL | 2.1371 mL | 4.2742 mL | 10.6856 mL | |
10 mM | 0.2137 mL | 1.0686 mL | 2.1371 mL | 5.3428 mL | |
20 mM | 0.1069 mL | 0.5343 mL | 1.0686 mL | 2.6714 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。
Pelitinib 257933-82-7 Angiogenesis JAK/STAT signaling MAPK Tyrosine Kinase/Adaptors MEK Src Raf EGFR inhibit 培利替尼 EKB569 HER1 Epidermal growth factor receptor Inhibitor WAY-EKB-569 ErbB-1 WAY-EKB569 EKB 569 EKB-569 WAY-EKB 569 inhibitor