货号 | 3580/50 |
别名 | (2E)-N-[[4-[[(3-Chloro-4-[(3-fluoro |
供应商 | Tocris |
生物活性 | 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. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 574.05 |
分子式 | C31H29ClFN5O |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 25 mM in ethanol |
参考文献 | Schifferet al (2007) Pharmacology and signaling properties of epidermal growth factor receptor isoforms studied by bioluminescence resonance energy transfer. Mol.Pharmacol. 71 508. PMID: 16968809. Kwaket al (2005) Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc.Natl.Acad.Sci.USA 102 7665. PMID: 15897464. Tsouet 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. |