吉非替尼-d6 (ZD1839-d6) 是氘标记的吉非替尼。 Gefitinib (ZD1839) 是一种有效的、选择性的、具有口服活性的 EGFR 酪氨酸激酶抑制剂，IC50 为 33 nM。 Gefitinib 选择性抑制 EGF 刺激的肿瘤细胞生长（IC50 为 54 nM）并阻断肿瘤细胞中 EGF 刺激的 EGFR 自磷酸化。吉非替尼还诱导自噬。吉非替尼具有抗肿瘤活性。
货号:ajcx22556
CAS:1228664-49-0
分子式:C22H18ClD6FN4O3
分子量：452.9
溶解度:DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 0.3 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Gefitinib-d₆is intended for use as an internal standard for the quantification of gefitinib by GC- or LC-MS. Gefitinib is a selective EGFR-TK inhibitor that blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC₅₀s ranging between 0.2-0.4 µM.¹By interfering with the intracellular kinase domain, gefitinib prevents EGFR autophosphorylation and prevents downstream signal transduction. Formulations containing gefitinib were previously used to treat advanced (or recurrent) non-small cell lung cancer. However, the FDA retracted its general approval when a phase III trial failed to demonstrate an overall survival benefit.²Formulations containing gefitinib appear to be most efficacious in treating certain EGFR gene mutations prevalent in Asian populations.^3,4

1.Ciardiello, F., Caputo, R., Bianco, R., et al.Antitumor effect and potentiation of cytotoxic drugs activity in human cancer cells by ZD-1839 (Iressa), an epidermal growth factor receptor-selective tyrosine kinase inhibitorClin. Cancer Res.6(5)2053-2063(2000) 2.Gerber, D.E.EGFR inhibition in the treatment of non-small cell lung cancerDrug Dev. Res.69(6)359-372(2008) 3.Yang, C.T., Hung, J.Y., Lai, C.L., et al.Gefitinib as first-line therapy for advanced or metastatic non-small cell lung cancer patients in southern TaiwanKaohsiung J. Med. Sci.26(1)1-7(2010) 4.Uruga, H., Kishi, K., Fujii, T., et al.Efficacy of gefitinib for elderly patients with advanced non-small cell lung cancer harboring epidermal growth factor receptor gene mutations: A retrospective analysisIntern. Med.49(2)103-107(2010)