Gefitinib是一种EGFR抑制剂，作用于NR6wtEGFR和NR6W细胞中的Tyr1173、Tyr992、Tyr1173和Tyr992，IC50 分别为37 nM、37nM、26 nM和57 nM。Gefitinib 可通过阻滞PI3K/AKT/mTOR信号通路来促进肺癌细胞的自噬和细胞凋亡。
| CAS No. | 184475-35-2 |
| 生物活性 | Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity. |
| 分子式 | C22H24ClFN4O3 |
| 分子量 | 446.9 |
| 储存条件 | Powder -20℃ 3 years |
| 溶解性数据 | DMSO : 250 mg/mL (559.41 mM; Need ultrasonic) |
| 体内研究 | Gefitinib (150 mg/kg, p.o.) in conbination with 1,1-Dimethylbiguanide induces a significant reduction in tumor growth in nude mice bearing H1299 or CALU-3 GEF-R cells that are grown subcutaneously as tumor xenografts. In irradiated rats, Gefitinib treatment augmentes lung inflammation, including inflammatory cell infiltration and pro-inflammatory cytokine expression, while Gefitinib treatment attenuates fibrotic lung remodeling due to the inhibition of lung fibroblast proliferation. |
| 体外研究 | Gefitinib (0.01-0.1 μM) results in increased phosphotyrosine load of the receptor, increased signalling to ERK and stimulation of proliferation and anchorage-independent growth, presumably by inducing EGFRvIII dimerisation in long-term exposure of EGFRvIII-expressing cells. On the other hand, gefitinib (1-2 μM) significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth. Gefitinib (ZD1839) inhibits the monolayer growth of these EGF-driven untransformed cells with IC50 of 20 nM. Gefitinib leads to an inhibition of CALU-3 and GLC82 cell proliferation, with an IC50 of 2 μM. |
| 文献 | 暂无相关参考文献 |
| 纯度及产品资料 | 98% |
邮箱：info@TianyaBio.com
电话：020-3107 8154
地址：广州市番禺区兴业大道东路1078号2-50
微信公众号
微信客服
