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Submit ReviewPelitinib
说明： Potent and irreversible EGFR inhibitor; orally bioavailable
别名： EKB-569
化学名： (2E)-N-[4-[(3-Chloro-4-fluorophenyl)amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
纯度： ≥97% (HPLC)
生物活性 for Pelitinib
Pelitinib 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.
许可信息
Sold for research purposes under agreement from Pfizer Inc
化合物库 for Pelitinib
Pelitinib is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for Pelitinib
| 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.
溶解性数据 for Pelitinib
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 23.4 | 50 |
制备储备液 for Pelitinib
以下数据基于产品分子量 467.92。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.27 mL | 21.37 mL | 42.74 mL |
| 2.5 mM | 0.85 mL | 4.27 mL | 8.55 mL |
| 5 mM | 0.43 mL | 2.14 mL | 4.27 mL |
| 25 mM | 0.09 mL | 0.43 mL | 0.85 mL |
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产品说明书 for Pelitinib
参考文献 for Pelitinib
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
If you know of a relevant reference for Pelitinib, please let us know.
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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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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.