MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
CAS No. : 184475-35-2
MCE 国际站:Gefitinib
产品活性:Gefitinib (ZD1839) 是一种有效,选择性和口服活性的 EGFR 酪氨酸激酶抑制剂,IC50 为 33 nM。Gefitinib 选择性抑制 EGF 刺激的肿瘤细胞生长 (IC50 为 54 nM),并阻断 EGF 刺激的肿瘤细胞中 EGFR 自磷酸化。Gefitinib 还可诱导细胞自噬 (autophagy) 和凋亡 (apoptosis),可用于癌症相关的研究,如肺癌和乳腺癌。
研究领域:JAK/STAT Signaling | Protein Tyrosine Kinase/RTK | Autophagy | Apoptosis
作用靶点:EGFR | Autophagy | Apoptosis
In Vitro: Gefitinib (0.01-0.1 μM, 72 h) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth.
Gefitinib (1-2 μM, 72 h) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth.
Gefitinib (0.62 μM, 24-72 h) inhibits IL-13-induced M2-like polarization of RAW 264.7 cells through the STAT6-dependent signaling pathway.
Gefitinib (0.62 μM, 72 h) inhibits M2-like macrophage-promoted invasion and migration.
Gefitinib (0-10 μM, 72 h) induces apoptosis (induction of BIM protein) in NSCLC Cell Lines (H3255 and HCC827 cells).
Gefitinib (100 nM, 24 h) suppresses macropinocytosis and increases the cellular uptake of extracellular vesicles( EVs) in HCC827 and A549 cells.
Gefitinib (1.5-60 μM, 48 h) increases inhibition of proliferation in H358R and A549R cells (Cisplatin-resistant wtEGFR NSCLC cell lines).
In Vivo: Gefitinib (Oral administration, 75 mg/kg/d, 21 days) inhibits the M2-like polarization of macrophages in LLC mice metastasis model.Gefitinib (Oral administration, 75 mg/kg for the initial week, daily for 5 consecutive days per week) eliminates phosphorylation of HER2 and HER3 and signaling through MAPK and Akt in lobular hyperplasias and carcinomas, increases MAPK activity and cytokine production in splenocytes and lymph nodes.Gefitinib (Oral gavage, 150 mg/kg, daily) enhances the anti-tumor effect of Cisplatin in H358R xenograft.
相关产品:Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | Apoptosis Compound Library | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | FDA-Approved Drug Library | Anti-Cancer Compound Library | CNS-Penetrant Compound Library | Autophagy Compound Library | Drug Repurposing Compound Library | Differentiation Inducing Compound Library | Anti-COVID-19 Compound Library | NMPA-Approved Drug Library | Orally Active Compound Library | FDA Approved & Pharmacopeial Drug Library | Anti-Hepatitis C Virus Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Drug-Induced Liver Injury (DILI) Compound Library | Anti-Pancreatic Cancer Compound Library | Targeted Therapy Drug Library | Anti-Obesity Compound Library | Angiogenesis-Related Compound Library | Anti-Liver Cancer Compound Library | Rare Diseases Drug Library | Anti-Colorectal Cancer Compound Library | EMA-Approved Drug Library | FDA-Approved Anticancer Drug Library | Human Metabolite Library | Anti-Prostate Cancer Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Off-patent Drug Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Mitochondrial Toxicity Compound Library | Highly Selective Inhibitors Library | Highly Selective Activators Library | SY-5609 | BRD4 Inhibitor-18 | 8α-Tigloyloxyhirsutinolide 13-O-acetate | AAPK-25 | Dutasteride-13C6 | Oleic acid-13C | Anticancer agent 120 | Abacavir sulfate | Meloxicam-d3-1 | Thailanstatin D | SB-218078 | Toyocamycin | Sorafenib-d4 | Busulfan | PTC-028 | Dinaciclib | EGFR/HER2/CDK9-IN-2 | CR-1-31-B | Lapatinib ditosylate | 142I5 | Farudodstat | Ecteinascidin 770 | BMS-690514 | AT9283 | Staurosporine | SNS-032 | AZA1 | Antitumor agent-96 | Erlotinib-d6 hydrochloride | Bleomycin A5
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库,我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物;
• 50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领;
• 产品种类涵盖各种重组蛋白,多肽,常用试剂盒 ,更有 PROTAC、ADC 等特色产品,广泛应用于新药研发、生命科学等科研项目;
• 提供虚拟筛选,离子通道筛选,代谢组学分析检测分析,药物筛选等专业技术服务;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果;
• 专业团队跟踪最新的制药及生命科学研究进展,为您提供全球最新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。