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化學性質:
規(guī)格 | 100mg 250mg |
CAS | 184475-55-6 |
別名 | Iressa hydrochloride;ZD 1839 hydrochloride;ZD-1839 hydrochloride;ZD1839 hydrochloride |
化學名 | N-(3-chloro-4-fluorophenyl)-7-methoxy-6-(3-morpholin-4-ylpropoxy)quinazolin-4-amine;hydrochloride |
分子式 | C22H25Cl2FN4O3 |
分子量 | 483.36 |
溶解度 | ≥ 6.9 mg/mL in DMSO with gentle warming, ≥ 4.28 mg/mL in H2O with ultrasonic and warming |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
The EGFR is a Mr 170,000 transmembrane glycoprotein with an external binding domain and an intracellular tyrosine kinase domain. Gefitinib (ZD-1839, Iressa) is an Epidermal Growth Factor Receptor-selective Tyrosine Kinase Inhibitor.
In vitro: Gefitinib inhibited colony formation in soft agar in a dose dependent manner in all cancer cell lines. However, treatment with higher doses resulted in a 2–4-fold increases in apoptosis. Dose-dependent supra-additive increase in growth inhibition was observed when cancer cells were treated with totoxic drugs and Gefitinib. The combined treatment markedly enhanced apoptotic cell death induced by single agent treatment [1].
In vivo: Gefitinib treatment of nude mice bearing established human GEO colon cancer xenografts revealed a reversible dose-dependent inhibition of tumor growth because GEO tumors resumed the growth rate of controls at the end of the treatment [1].
Clinical trial: Administration of a 250-mg dose of gefitinib as a dispersion preparation by drink or nasogastric tube achieved a systemic exposure to gefitinib that was consistent with that achieved when gefitinib was administered as a whole tablet. No evidence of tolerability problems associated with the routes of administration studied was observed in these healthy volunteers [2].
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原創(chuàng)作者:上海莼試生物技術有限公司
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