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Submit ReviewPelitinib is a potent irreversible EGFR inhibitor (IC50 = 20-80 nM). Selective for EGFR over Src, MEK/ERK, erbB2, Raf, c-Met and Cdk4 (IC50 values are 282, 800, 1255, 3353, 4100 and >20,000). Inhibits the growth of tumors overexpressing EGFR in vivo. Orally bioavailable.
Sold for research purposes under agreement from Pfizer Inc
Pelitinib is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 467.92 |
公式 | C24H23ClFN5O2 |
储存 | Store at -20°C |
纯度 | ≥97% (HPLC) |
CAS Number | 257933-82-7 |
PubChem ID | 6445562 |
InChI Key | WVUNYSQLFKLYNI-AATRIKPKSA-N |
Smiles | O=C(/C=C/CN(C)C)NC1=C(OCC)C=C(N=CC(C#N)=C2NC3=CC=C(F)C(Cl)=C3)C2=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Nunes et al (2004) Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human Mol.Cancer Ther. 3 21 PMID: 14749472
Hegedüs (2012) Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: Implications for the emergence and reversal of cancer drug resistance Biochem. Pharmacol. 84 260 PMID: 22548830
Tyner et al (2006) Blocking airway mucous cell metaplasia by inhibiting EGFR antiapoptosis and IL-13 transdifferentiation signals. J.Clin.Invest. 116 309 PMID: 16453019
Torrance et al (2000) Combinatorial chemoprevention of intestinal neoplasia. Nat.Med. 6 1024 PMID: 10973323
关键词: Pelitinib, Pelitinib supplier, EKB-569, orally, active, potent, irreversible, EGFR, inhibitors, inhibits, ErbB-1, in, vivo, 6349, Tocris Bioscience
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