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。

Osimertinib dimesylate

CAS No. : 2070014-82-1

MCE 国际站：Osimertinib dimesylate

产品活性：Osimertinib dimesylate (AZD-9291 dimesylate) 是不可逆的突变体选择性 EGFR 抑制剂；对EGFR^L858R 和EGFR^L858R/T790M 的 IC₅₀ 值分别为12 和 1 nM。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：EGFR

In Vitro: Osimertinib (AZD-9291) shows similar potency to early generation tyrosine kinase inhibitor (TKIs) in inhibiting EGFR phosphorylation in EGFR cells harboring sensitising EGFR mutants including PC-9 (ex19del), H3255 (L858R) and H1650 (ex19del), with mean IC₅₀ values ranging from 13 to 54 nM for Osimertinib (AZD-9291). Osimertinib (AZD-9291) also potently inhibits phosphorylation of EGFR in T790M mutant cell lines (H1975 (L858R/T790M), PC-9VanR (ex19del/T790M), with mean IC₅₀ potency less than 15 nM.

In Vivo: The tumor-bearing mice are treated with Osimertinib (AZD-9291) (5 mg/kg/day) for one to two weeks. Within days of treatment, 5 of 5 C/L858R mice displays nearly 80% reduction in tumor volume by magnetic resonance imaging MRI after therapy with Osimertinib (AZD-9291), while 5 of 5 mice treated with vehicle shows tumor growth. Osimertinib (AZD-9291) demonstrates improved rat PK, reduced hERG affinity, and improved IGF1R margins relative to the previously described compounds, and so this compound is selected for further investigation. Osimertinib (AZD-9291) also offers an additional degree of broader chemical and profile diversity when compared to the previously described lead compounds. Upon dosing Osimertinib (AZD-9291) in three efficacy models, The comparable efficacy is observed at relatively low doses (10 mg/kg per day). The excellent efficacy is also observed when Osimertinib (AZD-9291) is dosed at 5 mg/kg per day.

相关产品：Covalent Screening Library Plus  |  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  |  Covalent Screening Library  |  Differentiation Inducing Compound Library  |  Anti-diabetic Compound 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  |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  Highly Selective Inhibitors Library  |  Cytokine Inhibitors Library  |  Anti-Ovarian Cancer Compound Library  |  Multi-Target 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。