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。

Pelitinib

CAS No. : 257933-82-7

MCE 站：Pelitinib

产品活性：Pelitinib (EKB-569;WAY-EKB 569) 是可逆的 EGFR 抑制剂，IC₅₀ 值为38.5 nM。也可轻微抑制Src，MEK/ERK 和 ErbB2，IC₅₀ 值分别为282，800，和1255 nM。

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

作用靶点：EGFR  |  Src

In Vitro: Pelitini has much greater inhibitory activity against the EGFR kinase than against Src, MEK/ERK, Cdk4, c-Met, Raf and ErbB2, for example, the IC₅₀ for EGFR is 32-fold lower than the IC₅₀ for the closely related ErbB2. Pelitinib results in a dramatic reduction in EGFR phosphorylation but no change in the total amount of EGFR protein. It requires at least 10-fold more drug to equivalently inhibit ErbB2 phosphorylation in similar assays, and EKB-569 does not block phosphorylation of another receptor tyrosine kinase (c-Met) assessed in the same manner. EKB-569 is a potent inhibitor of proliferation in NHEK, A431, and MDA-468 cells (IC₅₀=61, 125, and 260 nM, respectively) but not MCF-7 cells (IC₅₀=3600 nM). EKB-569 is also a potent inhibitor of EGF-induced phosphorylated EGF-R (pEGF-R) in A431 and NHEK cells (IC₅₀=20-80 nM).

In Vivo: A single oral dose of 10 mg/kg EKB-569 inhibits EGFR phosphorylation in A431 xenografts within 60 minutes. Twenty-four hours later, EGFR activity is still inhibited by over 50% by this single oral dose. The half-life of EKB-569 in mouse plasma is about 2 hours.

相关产品：Covalent Screening Library Plus  |  Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Covalent Screening Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-Hepatitis C Virus Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Gefitinib  |  Trastuzumab  |  Erlotinib  |  Cetuximab  |  AG490  |  Genistein  |  Bosutinib  |  PP2  |  AG-1478  |  Pertuzumab  |  BI-4020  |  SU6656  |  NSC 228155  |  Src Inhibitor 1  |  WH-4-023  |  Scutellarein  |  Mubritinib  |  TX1-85-1  |  PP1  |  1-Naphthyl PP1  |  1-NM-PP1  |  Canertinib  |  Lck Inhibitor  |  Butein  |  PD168393  |  Daphnetin  |  EGFR-IN-7

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 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；
•   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 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*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。