| 中文名称： | 盐酸吉非替x | 中文别名： | 盐酸吉非替x |
|---|---|---|---|
| 英文名称： | Gefitinib Hydrochloride | CAS： | 184475-55-6 |
| 产品分类： | 小分子化合物 | 纯度： | ≥98% |
| 产品编号 | 品牌 | 纯度 | 规格 | 库存 | 价格 |
|---|---|---|---|---|---|
| IG1500 | 索莱宝 | ≥98% | 100mg | 有现货 | 540.00 元 |
| IG1500 | 索莱宝 | ≥98% | 500mg | 有现货 | 940.00 元 |
| 标准名称: | 盐酸吉非替x | 英文名称： | Gefitinib hydrochloride |
|---|---|---|---|
| CAS： | 184475-55-6 | 分子式： | C22H25Cl2FN4O3 |
| 分子量： | 483.363306760788 | 颜色与性状： | |
| 密度： | 沸点： | 607.7°C at 760 mmHg | |
| 熔点： | 水溶性： |
| CAS | 184475-55-6 |
| 中文名称 | 盐酸吉非替x |
| 英文名称 | Gefitinib Hydrochloride |
| 分子式 | C22H25Cl2FN4O3 |
| 分子量 | 483.36 |
| 规格 | 100mg ; 500mg |
| 溶解性 | Soluble in Water |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| 运输条件 | 冷藏运输 |
| MDL | MFCD00952718 |
| SMILES | COC1=C(C=C2C(=C1)N=CN=C2NC3=CC(=C(C=C3)F)Cl)OCCCN4CCOCC4.Cl |
| InChIKey | QUINXWLATMJDQF-UHFFFAOYSA-N |
| InChI | InChI=1S/C22H24ClFN4O3.ClH/c1-29-20-13-19-16(12-21(20)31-8-2-5-28-6-9-30-10-7-28)22(26-14-25-19)27-15-3-4-18(24)17(23)11-15;/h3-4，11-14H，2，5-10H2，1H3，(H，25，26，27);1H |
| PubChem CID | 19077490 |
| 靶点 | EGFR |
| 通路 | Angiogenesis;Protein Tyrosine Kinase/RTK |
| 背景说明 | Gefitinib Hydrochloride是一种有效的 EGFR tyrosine kinase 抑制剂。 |
| 生物活性 | Gefitinib hydrochloride (ZD1839 hydrochloride) is a potent， selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib hydrochloride selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib hydrochloride also induces autophagy. Gefitinib hydrochloride has antitumour activity.[1-5] |
| In Vitro | Gefitinib (0.01-0.1 mM) 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 mM) significantly decreases EGFRvIII phosphotyrosine load， EGFRvIII-mediated proliferation and anchorage-independent growth[1]. Gefitinib (ZD1839) inhibits the monolayer growth of these EGF-driven untransformed cells with IC50 of 20 nM[2]. Gefitinib leads to an inhibition of CALU-3 and GLC82 cell proliferation， with an IC50 of 2 μM[3]. |
| In Vivo | Gefitinib (150 mg/kg， p.o.) in conbination with Metformin 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[3]. 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[4]. |
| 细胞实验 | Cancer cells are seeded in 96-well plates and are treated with different doses of Gefitinib (0.01-20 μM)， Metformin or both for 72 hours. Cell proliferation is measured with the MTT assay. The IC50 values are determined by interpolation from the dose-response curves. Results represent the median of 3 separate experiments each conducted in quadruplicate. The results of the combined treatment are analyzed according to the method of Chou and Talalay by using the CalcuSyn software program[3]. |
| 动物实验 | Mice[3] Four- to 6-week old female balb/c athymic (nu+/nu+) mice are acclimatized for 1 week before being injected with cancer cells and injected subcutaneously with 107 H1299 and CALU-3 GEF-R cells that has been resuspended in 200 μL of Matrigel. When established tumors of approximately 75 mm3 in diameter are detected， mice are left untreated or treated with oral administrations of metformin (200 mg/mL metformin diluted in drinking water and present throughout the experiment)， gefitinib (150 mg/kg daily orally by gavage)， or both for the indicated time periods. Each treatment group consists of 10 mice. Tumor volume is measured using the formula π/6×larger diameter×(smaller diameter)2. Rats[4] The rats are randomly assigned to 1 of 4 experimental groups: 1) the unirradiated rats treated with oral administration of vehicle (0.1% Tween 80) once daily; 2) the unirradiated rats treated with oral administration of gefitinib (50 mg/kg/day) once daily; 3) the irradiated rats treated with oral administration of vehicle once daily; 4) the irradiated rats treated with oral administration of gefitinib once daily. Each experimental group comprised 5-6 rats and all treatments are delivered for 14 days. |
| 数据来源文献 | [1]. Wakeling AE， et al. ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 2002 Oct 15;62(20):5749-54. [2]. Pedersen MW， et al. Differential response to gefitinib of cells expressing normal EGFR and the mutant EGFRvIII. Br J Cancer. 2005 Oct 17;93(8):915-23. [3]. Moasser MM， et al. The tyrosine kinase inhibitor ZD1839 (“Iressa“) inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells. Cancer Res. 2001 Oct 1;61(19):7184-8. [4]. Morgillo F， et al. Synergistic effects of metformin treatment in combination with gefitinib， a selective EGFR tyrosine kinase inhibitor， in LKB1 wild-type NSCLC cell lines. Clin Cancer Res. 2013 Jul 1;19(13):3508-19. [5]. Miyake K， et al. Epidermal growth factor receptor-tyrosine kinase inhibitor (gefitinib) augments pneumonitis， but attenuates lung fibrosis in response to radiation injury in rats. J Med Invest. 2012;59(1-2):174-85. |
| 单位 | 瓶 |
| 1mM-5mg | 10.3443mL |
| 1mM-1mg | 2.0689mL |
| 1mM-10mg | 20.6885mL |
| 5mM-1mg | 0.4138mL |
| 5mM-5mg | 2.0689mL |
| 5mM-10mg | 4.1377mL |
| 10mM-1mg | 0.2069mL |
| 10mM-5mg | 1.0344mL |
| 10mM-10mg | 2.0689mL |
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| 企业认证： | 已认证 | 企业性质： | 生产研发 |
|---|---|---|---|
| 主营产品： | 硫酸链霉素水溶液(50mg/ml,无菌） ； 盐酸四环素无菌水溶液(5mg/ml） ； Pronase E ； 10mg/ml杀稻瘟菌素 S(无菌，<1EU/mg) ； 硫酸葡聚糖钠盐(结肠炎造模用DSS) ； | 供货范围： | 试剂 |
| 产品目录： | 119905 | 品牌： | 索莱宝 |
| 纯度 | 品牌 | 规格 | 发货地 |
|---|---|---|---|
| - | 索莱宝 | 10ml | 北京 |
| 纯度 | 品牌 | 规格 | 发货地 |
|---|---|---|---|
| - | 索莱宝 | 10ml | 北京 |
