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。
Gefitinib hydrochloride
CAS No. : 184475-55-6
MCE 国际站：Gefitinib hydrochloride
产品活性：Gefitinib hydrochloride (ZD1839 hydrochloride) 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 hydrochloride 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 hydrochloride 还可诱导细胞自噬 (autophagy)，并具有抗肿瘤活性。
研究领域：JAK/STAT Signaling | Protein Tyrosine Kinase/RTK
作用靶点：EGFR
In Vitro: Gefitinib (0.01-0.1 mM) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth, presumably by inducing EGFRvIII dimerisation in long-term exposure of EGFRvIII-expressing cells. On the other hand, gefitinib (1-2 mM) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth. Gefitinib (ZD1839) inhibits the monolayer growth of these EGF-driven untransformed cells with IC50 of 20 nM. Gefitinib leads to an inhibition of CALU-3 and GLC82 cell proliferation, with an IC50 of 2 μM.
In Vivo: Gefitinib (150 mg/kg, p.o.) in conbination with Metformin induces a significant reduction in tumor growth in nude mice bearing H1299 or CALU-3 GEF-R cells that are grown subcutaneously as tumor xenografts. In irradiated rats, Gefitinib treatment augmentes lung inflammation, including inflammatory cell infiltration and pro-inflammatory cytokine expression, while Gefitinib treatment attenuates fibrotic lung remodeling due to the inhibition of lung fibroblast proliferation.
相关产品：Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | FDA-Approved Drug Library | Anti-Cancer 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-Lung Cancer Compound Library | Drug-Induced Liver Injury (DILI) Compound Library | Anti-Pancreatic Cancer Compound 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 | Highly Selective Inhibitors Library | Cytokine Inhibitors Library | Anti-Ovarian Cancer Compound Library | Bioactive Compound Library Max | Osimertinib | Trastuzumab | Gefitinib | Cetuximab | Erlotinib | Afatinib | Trastuzumab deruxtecan | Lapatinib | Genistein | AG490 | Trastuzumab emtansine | Neratinib | Tucatinib | Dacomitinib | Disitamab vedotin | Pertuzumab | AG-1478 | Amivantamab | NSC 228155 | Patritumab | Mobocertinib | Panitumumab | Pyrotinib | Sapitinib | Firmonertinib mesylate | BLU-945 | Lazertinib
热门产品线：重组蛋白 | 药物筛选 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物
Trending products：Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Dye Reagents | PROTAC | Isotope-Labeled Compounds
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域；
• 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。
