Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PD158780是一种EGFR 家族抑制剂,对EGFR、ErbB2、ErbB3和ErbB4的IC50值分别为8 μM、49、52 和 52 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 239 | 现货 | ||
5 mg | ¥ 540 | 现货 | ||
10 mg | ¥ 930 | 现货 | ||
25 mg | ¥ 2,060 | 现货 | ||
50 mg | ¥ 3,400 | 现货 | ||
100 mg | ¥ 4,930 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 540 | 现货 |
产品描述 | PD 158780 reversibly inhibits auto and transphosphorylation of all four members of the ErbB receptor superfamily: EGFR, ErbB2, ErbB3, and ErbB4 (IC50s: 8μM, 49 nM, 52 nM, and 52 nM in cell assay). |
靶点活性 | EGFR:0.008 nM (cell free), EGFR:8 μM (Cell Assay), ERB4:52 nM (Cell Assay), ErbB2:49 nM (Cell Assay), ERB3:52 nM (Cell Assay) |
体外活性 | PD158780 inhibited EGF receptor autophosphorylation in A431 human epidermoid carcinoma with IC50 values of 13 nM. PD 158780 was highly specific for the EGF receptor in Swiss 3T3 fibroblasts, inhibiting EGF-dependent receptor autophosphorylation and thymidine incorporation at low nanomolar concentrations. PD 158780 inhibited heregulin-stimulated phosphorylation in the SK-BR-3 and MDA-MB-453 breast carcinomas with IC50 values of 49 and 52 nM, respectively [1]. |
激酶实验 | Epidermal growth factor receptor was prepared from human A431 carcinoma cell shed membrane vesicles by immunoaffinity chromatography as previously described, and the assays were carried out as reported previously. The substrate used was based on a portion of phospholipase Cγ1, having the sequence Lys-His-Lys-Lys-LeuAla-Glu-Gly-Ser-Ala-Tyr472-Glu-Glu-Val. The reaction was allowed to proceed for 10 min at room temperature and then was stopped by the addition of 2 mL of 75 mM phosphoric acid. The solution was then passed through a 2.5 cm phosphocellulose disk which bound the peptide. This filter was washed with 75 mM phosphoric acid (5×), and the incorporated label was assessed by scintillation counting in an aqueous fluor. Control activity (no drug) gave a count of approximately 100 000 cpm. At least two independent dose-response curves were done and the IC50 values computed. The reported values are averages; variation was generally ±15% [1]. |
细胞实验 | All cell lines were maintained as monolayers in dMEM/F12, 50:50 containing 10% fetal bovine serum. For growth inhibition assays, dilutions of the designated compound in 10 μL were placed in 24-well Linbro plates (1.7 x 1.6 cm, flat bottom) followed by the addition of cells (2 × 10^4) in 2 mL of medium. The plates were incubated for 72 hr at 37 °C in a humidified atmosphere containing 5% CO 2 in air. Cell growth was determined by counting cells with a Coulter model AM electronic cell counter. For clone formation in soft agar, cells were trypsinized, and 10,000 cells/mL were seeded into DMEM/F12 medium containing 10% fetal bovine serum, 0.4% agarose, and the designated concentration of compound. One milliliter of this solution was placed over a bottom layer of the same medium containing 0.8% agarose in a 35-mm Petri dish and incubated at 37 °C in a humidified atmosphere containing 5% CO 2 in air. After 3 weeks, colonies were stained with p-iodonitrotetrazolium violet (INT) and quantitated with an image analyzer using the software NIH Image version 1.55. Incorporation of radiolabeled thymidine into cellular DNA was monitored by exposing compound-treated or control cells to [methyl)H]thymidine at a concentration of 1 μM and specific activity of 1 μCi/nmol. After 2 hr the cells were trypsinized and injected into 2 mL of ice-cold 15% trichloroacetic acid (TCA). The resulting precipitate was collected on glass fiber filters, washed five times with 2-mL aliquots of ice-cold 15% TCA, dried, and placed in scintillation vials plus 10 mL Ready gel [1]. |
分子量 | 330.18 |
分子式 | C14H12BrN5 |
CAS No. | 171179-06-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 8 mg/mL (24.23 mM)
DMSO: 30 mg/mL (90.86 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 3.0287 mL | 15.1433 mL | 30.2865 mL | 75.7163 mL |
5 mM | 0.6057 mL | 3.0287 mL | 6.0573 mL | 15.1433 mL | |
10 mM | 0.3029 mL | 1.5143 mL | 3.0287 mL | 7.5716 mL | |
20 mM | 0.1514 mL | 0.7572 mL | 1.5143 mL | 3.7858 mL | |
DMSO | 50 mM | 0.0606 mL | 0.3029 mL | 0.6057 mL | 1.5143 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。
PD158780 171179-06-9 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Inhibitor PD 158780 Epidermal growth factor receptor inhibit PD-158780 HER1 ErbB-1 inhibitor