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Gefitinib

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产品编号 T1181Cas号 184475-35-2
别名 吉非替尼, ZD1839

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。

Gefitinib

Gefitinib

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纯度: 100%
产品编号 T1181 别名 吉非替尼, ZD1839Cas号 184475-35-2

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。

规格价格库存数量
50 mg¥ 163.5¥ 327现货
100 mg¥ 230¥ 460现货
500 mg¥ 399¥ 798现货
1 g¥ 589¥ 1,178现货
5 g¥ 1,180.5¥ 2,361现货
1 mL x 10 mM (in DMSO)¥ 248.5¥ 497现货
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产品介绍

生物活性
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].
别名吉非替尼, ZD1839
化学信息
分子量446.9
分子式C22H24ClFN4O3
CAS No.184475-35-2
SmilesN(C=1C2=C(C=C(OC)C(OCCCN3CCOCC3)=C2)N=CN1)C4=CC(Cl)=C(F)C=C4
密度1.322g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 18.33 mg/mL (41.02 mM)
Ethanol: 4.5 mg/mL (10 mM)
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4.47 mg/mL (10 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
溶液配制表
1mg5mg10mg50mg
1 mM2.2376 mL11.1882 mL22.3764 mL111.8819 mL
5 mM0.4475 mL2.2376 mL4.4753 mL22.3764 mL
10 mM0.2238 mL1.1188 mL2.2376 mL11.1882 mL

TCMIP相关数据

中药材来源及性味归经
中药材名称中药材拉丁名归经
雷公藤Tripterygium wilfordii Hook. f.辛, 苦心, 肝
所属中成药
中成药名称处方组成中成药类型
雷公藤片雷公藤清热药
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,黄芪扶正药
所属中药方剂
方剂名称处方组成剂型处方来源

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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