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Pelitinib
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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
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
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热门标签:EKB-569