O-Desmethyl gefitinib
Cat. No.:YN340331
| 产品名称: | O-Desmethyl gefitinib |
| CAS No.: | 847949-49-9 |
| Chemical Name: | 4-[(3-chloro-4-fluorophenyl)amino]-6-[3-(4-morpholinyl)propoxy]-7-quinazolinol |
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| 分子量: | 432.9 |
| 分子式: | C21H22ClFN4O3 |
| SMILES: | OC1=CC2=C(C(NC3=CC=C(F)C(Cl)=C3)=NC=N2)C=C1OCCCN4CCOCC4 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | O-Desmethyl gefitinib 是 Gefitinib 在人血浆中的活性代谢产物。O-Desmethyl gefitinib 的形成依赖于 CYP2D6 活性。在亚细胞试验中,O-Desmethyl gefitinib 抑制EGFR,IC50为 36 nM。 |
| IC50和靶点: | |
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McKillop, D., Hutchison, M., Partridge, E.A., et al.Metabolic disposition of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat, dog and manXenobiotica34(10),917-934(2004)
McKillop, D., Guy, S.P., Spence, M.P., et al.Minimal contribution of desmethyl-gefitinib, the major human plasma metabolite of gefitinib, to epidermal growth factor receptor (EGFR)-mediated tumour growth inhibitionXenobiotica36(1),29-39(2006)
Kobayashi, H., Sato, K., Niioka, T., et al.Effects of polymorphisms in CYP2D6 and ABC transporters and side effects induced by gefitinib on the pharmacokinetics of the gefitinib metabolite, O-desmethyl gefitinibMed. Oncol.33(6),1-8(2016)