化合物 PD158780,PD158780
  • 化合物 PD158780,PD158780

化合物 PD158780|T5410|TargetMol

价格 143 323 558
包装 1mg 5mg 10mg
最小起订量 1mg
发货地 上海
更新日期 2024-09-29
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产品详情

中文名称:化合物 PD158780英文名称:PD158780
CAS:171179-06-9品牌: TargetMol
产地: 美国保存条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格: 98.81%产品类别: 抑制剂
货号: T5410
2024-09-29 化合物 PD158780 PD158780 1mg/143RMB;5mg/323RMB;10mg/558RMB 143 TargetMol 美国 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 98.81% 抑制剂

Product Introduction

Bioactivity

名称PD158780
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).
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].
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].
体外活性PD158780在A431人类表皮样癌细胞中抑制了EGF受体的自磷酸化作用,IC50值为13 nM。PD158780对EGF受体具有很高的特异性,在Swiss 3T3成纤维细胞中,以低纳摩尔浓度抑制了依赖EGF的受体自磷酸化和胸腺嘧啶的掺入。PD158780还抑制了SK-BR-3和MDA-MB-453乳腺癌细胞中由heregulin刺激的磷酸化作用,IC50值分别为49 nM和52 nM [1]。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : 8 mg/mL (24.23 mM)
DMSO : 30 mg/mL (90.86 mM)
关键字Inhibitor | PD158780 | PD 158780 | Epidermal growth factor receptor | inhibit | PD-158780 | HER1 | EGFR | ErbB-1
相关产品Lapatinib | Neratinib | Chalcone | Gefitinib | Erlotinib | Osimertinib | Erlotinib hydrochloride | Afatinib Dimaleate | Lidocaine Hydrochloride hydrate | Genistein | Khellin | Osimertinib mesylate
相关库抑制剂库 | 血管生成库 | 经典已知活性库 | 已知活性化合物库 | 抗结直肠癌化合物库 | 激酶抑制剂库 | JAK-STAT 化合物库 | 抗卵巢癌化合物库 | 膜蛋白靶向化合物库 | 酪氨酸激酶分子库
关键字: PD158780|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。
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