Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Gefitinib (ZD1839) 是一种 EGFR 一代抑制剂,具有口服活性,抑制 EGFR 19 Del 和 L858R 突变。Gefitinib 具有抗肿瘤活性,用于治疗 EGFR 突变的非小细胞肺癌。Gefitinib 用药会产生 EGFR C797S 耐药突变。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
50 mg | ¥ 327 | 现货 | ||
100 mg | ¥ 460 | 现货 | ||
500 mg | ¥ 798 | 现货 | ||
1 g | ¥ 1,178 | 现货 | ||
5 g | ¥ 2,361 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 497 | 现货 |
产品描述 | Gefitinib (ZD1839) is an EGFR first-generation inhibitor with oral activity that inhibits the EGFR 19 Del and L858R mutations. Gefitinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Gefitinib administration RESULTS in the development of the EGFR C797S resistance mutation. |
靶点活性 | Tyr1173:26 nM (NR6W cells), Tyr1173:37 nM (NR6wtEGFR cells), Tyr992:37 nM (NR6wtEGFR cells) , Tyr992:57 nM (NR6W cells) |
体外活性 |
方法:23 种肿瘤细胞用 Gefitinib 处理 72 h,使用 MTT 方法检测细胞活力。
结果:只有 PC9 细胞系的 IC50<1 μmol/L (高度敏感),14 个细胞系的 IC50>10 μmol/L (抗性),其余 8 个细胞系具有 1-10 μmol/L 的 IC50 (中等敏感)。[1] 方法:肿瘤细胞 HT29、KB、Du145 和 A549 用 Gefitinib (0.032-50 μM) 处理 2 h,在细胞裂解前五分钟加入 EGF (0.1 μg/mL),使用 Western Blot 方法检测靶点蛋白表达水平。 结果:Gefitinib 在所有肿瘤细胞系中产生 EGFR 自磷酸化的剂量依赖性抑制。[2] |
体内活性 |
方法:为检测体内抗肿瘤活性,将 Gefitinib (3.125-200 mg/kg in 0.5% polysorbate 80) 口服给药给携带肿瘤 A431、 Du145 或 A549 的 nude 小鼠,每天一次,持续七-十五天。
结果:Gefitinib 剂量依赖性方式抑制 A431、 Du145 或 A549 肿瘤生长。[2] 方法:为检测体内抗肿瘤活性,将 Gefitinib (40 mg/kg,每天一次) 或 Gefitinib (200 mg/kg,每五天一次) 灌胃给药给携带人肺癌肿瘤 H3255 的 athymic nude 小鼠,持续两周。 结果:每周治疗显示出比每天治疗更好的抑制作用。与每日给药方案相比,每周给药方案对 p-EGFR、p-ERK 和 p-AKT 的抑制作用更强。[3] |
细胞实验 | The human NSCLC H1299, H1975, A549, H460, GLC82, H460, and CALU-3 cell lines were provided by the American Type Culture Collection and maintained in RPMI-1640 supplemented with 10% FBS in a humidified atmosphere with 5% CO2. CALU-3 GEF-R is a cell line obtained in vitro as previously described. Briefly, over a period of 12 months, human CALU-3 lung adenocarcinoma cells were continuously exposed to increasing concentrations of gefitinib. The starting dose was the dose causing the inhibition of 50% of cancer cell growth (IC50; gefitinib, 1 μmol/L). The drug dose was progressively increased to 15 μmol/L in approximately 2 months, to 20 μmol/L after other 2 months, to 25 μmol/L after additional 2 months, and, finally, to 30 μmol/L for a total of 12 months. The established resistant cancer cell lines were then maintained in continuous culture with the maximally achieved dose of each TKI that allowed cellular proliferation (30 μmol/L for each drug) [2]. |
动物实验 | Four- to 6-week old female balb/c athymic (nu+/nu+) mice were purchased from Charles River Laboratories. Mice were acclimatized for 1 week before being injected with cancer cells and injected subcutaneously with 107 H1299 and CALU-3 GEF-R cells that had been resuspended in 200 μL of Matrigel. When established tumors of approximately 75 mm3 in diameter were detected, mice were 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 consisted of 10 mice. Tumor volume was measured using the formula π/6 × larger diameter × (smaller diameter)2. Tumor tissues were collected from the xenografts and analyzed by Western blotting for the expression and activation of EGFR, AMPK, mitogen-activated protein kinase (MAPK), and S6 [2]. |
别名 | ZD1839, 吉非替尼 |
化合物与蛋白结合的复合物 |
Complex structure of cyclin G-associated kinase with gefitinib |
分子量 | 446.9 |
分子式 | C22H24ClFN4O3 |
CAS No. | 184475-35-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 44.7 mg/mL (100 mM)
Ethanol: 4.5 mg/mL (10 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.2376 mL | 11.1882 mL | 22.3764 mL | 55.9409 mL |
5 mM | 0.4475 mL | 2.2376 mL | 4.4753 mL | 11.1882 mL | |
10 mM | 0.2238 mL | 1.1188 mL | 2.2376 mL | 5.5941 mL | |
DMSO | 20 mM | 0.1119 mL | 0.5594 mL | 1.1188 mL | 2.797 mL |
50 mM | 0.0448 mL | 0.2238 mL | 0.4475 mL | 1.1188 mL | |
100 mM | 0.0224 mL | 0.1119 mL | 0.2238 mL | 0.5594 mL |
中药材名称 | 中药材拉丁名 | 性 | 味 | 归经 |
雷公藤 | Tripterygium wilfordii Hook. f. | 凉 | 辛, 苦 | 心, 肝 |
中成药名称 | 处方组成 | 主治疾病 | 中成药类型 |
雷公藤片 | 雷公藤 | N/A | 清热药 |
金关片 | 雷公藤,续断,山药,细辛,制附子,茯苓,桑枝,桂枝,鹿角霜,秦艽,丹参,枸杞子,牛膝,鸡血藤,黄精,淫羊藿,薏苡仁,黄芪 | 口服,一次4片,一日3次。 | 扶正药 |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Gefitinib 184475-35-2 Angiogenesis Autophagy JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Tyrosine Kinases EGFR tyrosine kinase lung cancer breast cancer phosphorylation ZD1839 Inhibitor 吉非替尼 Apoptosis inhibit TAMs NSCLCs antitumour Epidermal growth factor receptor HER1 tumor metastasis ZD-1839 ZD 1839 ErbB-1 inhibitor