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说明： Dual irreversible inhibitor of ErbB2 and EGFR
化学名： (2E)-N-[[4-[[(3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
纯度： ≥98% (HPLC)
生物活性 for HKI 357
HKI 357 is a potent, irreversible inhibitor of ErbB2 (HER2) and EGFR (IC50 values are 33 and 34 nM respectively). Suppresses ligand-induced EGFR autophosphorylation and cell proliferation in NCI-H1975 cells containing L858R and T790M mutations. Circumvents mechanisms of resistance to Iressa (Cat. No. 3000) in non-small-cell lung cancer cells.
技术数据 for HKI 357
| 分子量 | 574.05 |
| 公式 | C31H29ClFN5O3 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 848133-17-5 |
| PubChem ID | 11238512 |
| InChI Key | NERXPXBELDBEPZ-RMKNXTFCSA-N |
| Smiles | O=C(/C=C/CN(C)C)NC1=C(OCC)C=C(N=CC(C#N)=C2NC3=CC=C(OCC4=CC=CC(F)=C4)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.
产品说明书 for HKI 357
参考文献 for HKI 357
参考文献是支持产品生物活性的出版物。
Kwak et al (2005) Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefi. Proc.Natl.Acad.Sci.USA 102 7665 PMID: 15897464
Tsou et al (2005) Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity. J.Med.Chem. 48 1107 PMID: 15715478
Schiffer et al (2007) Pharmacology and signaling properties of epidermal growth factor receptor isoforms studied by bioluminescence resonance energy transfer. Mol.Pharmacol. 71 508 PMID: 16968809
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关键词: HKI 357, HKI 357 supplier, HKI357, EGFR, epidermal, growth, factor, receptors, inhibitors, inhibits, irreversible, dual, potent, ErbB2, HER2, 3580, Tocris Bioscience
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.