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Gefitinib

Gefitinib

产品编号 T1181   CAS 184475-35-2
别名: ZD1839, 吉非替尼

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。

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Gefitinib Chemical Structure
Gefitinib, CAS 184475-35-2
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
其他形式的 Gefitinib:
产品目录号及名称: Gefitinib (T1181)
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纯度: 100%
纯度: 100%
纯度: 100%
纯度: 100%
纯度: 100%
纯度: 99.92%
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天然产物信息
生物活性
化学信息
存储 & 溶解度
TCMIP信息
参考文献
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

T1181_2

Complex structure of cyclin G-associated kinase with gefitinib

分子量 446.9
分子式 C22H24ClFN4O3
CAS No. 184475-35-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 44.7 mg/mL (100 mM)

Ethanol: 4.5 mg/mL (10 mM)

溶液配制表

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
TCMIP相关数据
中药材来源及性味归经
所属中成药

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 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

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
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Noro R, et al. Gefitinib (IRESSA) sensitive lung cancer cell lines show phosphorylation of Akt without ligand stimulation. BMC Cancer. 2006 Dec 6;6:277. 2. 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. 3. Zhang Q, et al. Effect of weekly or daily dosing regimen of Gefitinib in mouse models of lung cancer. Oncotarget. 2017 Aug 2;8(42):72447-72456. 4. Tan J, et al. Tyrosine kinase inhibitors show different anti-brain metastases efficacy in NSCLC: A direct comparative analysis of icotinib, gefitinib, and erlotinib in a nude mouse model. Oncotarget. 2017 Oct 19;8(58):98771-98781. 6. Dhar D, et al. Liver Cancer Initiation Requires p53 Inhibition by CD44-Enhanced Growth Factor Signaling. Cancer Cell. 2018 Jun 11;33(6):1061-1077.e6. 8. Teng J F, Qin D L, Mei Q, et al. Polyphyllin VI, a saponin from Trillium tschonoskii Maxim. induces apoptotic and autophagic cell death via the ROS triggered mTOR signaling pathway in non-small cell lung cancer[J]. Pharmacological Research. 2019: 104396. 9. . circSETD3 Contributes to Acquired Resistance to Gefitinib in Non-Small-Cell Lung Cancer by Targeting the miR-520h/ABCG2 Pathway. Molecular Therapy-Nucleic Acids. 2020 10. Quan C, Chen Y, Wang X, et al. Loss of histone lysine methyltransferase EZH2 confers resistance to tyrosine kinase inhibitors in non-small cell lung cancer. cancer letters. 2020

文献引用

1. Oeller M, Jaksch-Bogensperger H, Templin M, et al.Transcription Factors STAT3 and MYC Are Key Players of Human Platelet Lysate-Induced Cell Proliferation.International Journal of Molecular Sciences.2022, 23(24): 15782. 2. He S, Shi J, Zhou H H, et al.Lnc-ABCA12-8 confers acquired resistance to gefitinib in non-small cell lung cancer by regulating the alternative splicing of fibronectin 1 in the IIICS region.Cancer Gene Therapy.2022, 29(11): 1686-1696. 3. Wen C, Li Y, Huang Y, et al.CircSETD3 mediates acquired resistance to gefitinib in non-small lung cancer cells by FXR1/ECT2 pathway.The International Journal of Biochemistry & Cell Biology.2022: 106344. 4. Hu L, Liu Y, Fu C, et al.The Tumorigenic Effect of the High Expression of Ladinin-1 in Lung Adenocarcinoma and Its Potential as a Therapeutic Target.Molecules.2023, 28(3): 1103. 5. Chen J, Lei C, Nie D, et al.Inorganic arsenic exposure promotes malignant progression by HDAC6‐mediated down‐regulation of HTRA1.Journal of Applied Toxicology.2023 6. Jiao D, Chen Y, Liu X, et al.Targeting MET endocytosis or degradation to overcome HGF-induced gefitinib resistance in EGFR-sensitive mutant lung adenocarcinoma.Biochemical and Biophysical Research Communications.2023 7. Yang S, Yang S, Zhang H, et al. Targeting Na+/K+‐ATPase by berbamine and ouabain synergizes with sorafenib to inhibit hepatocellular carcinoma. British Journal of Pharmacology. 2021 8. Zhao X, Zhang N, Huang Y, et al. Lansoprazole Alone or in Combination With Gefitinib Shows Antitumor Activity Against Non-small Cell Lung Cancer A549 Cells in vitro and in vivo. Frontiers in Cell and Developmental Biology. 2021, 9: 947 9. Wang L, Liu X X, Yang Y M, et al. RHBDF2 gene functions are correlated to facilitated renal clear cell carcinoma progression. Cancer Cell International. 2021, 21(1): 1-18. 10. Shi J, Huang Y, Wen C, et al. Genome-wide identification and characterization of long non-coding RNAs involved in acquired resistance to gefitinib in non-small-cell lung cancer. Computational Biology and Chemistry. 2020, 87: 107288.
11. Zhao Deng,Chenbin Cui,Yanan Wang,Jiangjin Ni, et al. FSGHF3 and peptides, prepared from fish skin gelatin, exert a protective effect on DSS-induced colitis via the Nrf2 pathway. Food & Function. 2020 12. Cao D, Chen D, Xia J N, et al. Artesunate promoted anti-tumor immunity and overcame EGFR-TKI resistance in non-small-cell lung cancer by enhancing oncogenic TAZ degradation. Biomedicine & Pharmacotherapy. 2022, 155: 113705. 13. Liu Y, Luo Y, Yan S, et al. CRL2KLHDC3 mediates p14ARF N-terminal ubiquitylation degradation to promote non-small cell lung carcinoma progression. Oncogene. 2022: 1-14 14. Kang J, Guo Z, Zhang H, et al. Dual Inhibition of EGFR and IGF-1R Signaling Leads to Enhanced Antitumor Efficacy against Esophageal Squamous Cancer. International Journal of Molecular Sciences. 2022, 23(18): 10382 15. Teng J F, Qin D L, Mei Q, et al. Polyphyllin VI, a saponin from Trillium tschonoskii Maxim. induces apoptotic and autophagic cell death via the ROS triggered mTOR signaling pathway in non-small cell lung cancer. Pharmacological Research. 2019: 104396. 16. Shang J, Ning S, Chen Y, et al. MDL-800, an allosteric activator of SIRT6, suppresses proliferation and enhances EGFR-TKIs therapy in non-small cell lung cancer. Acta Pharmacologica Sinica. 2021, 42(1): 120-131 17. Zheng P, Huang Z, Tong D C, et al. Frankincense myrrh attenuates hepatocellular carcinoma by regulating tumor blood vessel development through multiple epidermal growth factor receptor-mediated signaling pathways. World Journal of Gastrointestinal Oncology. 2022, 14(2): 450 18. Yu J, Zhang L, Peng J, et al. Dictamnine, a novel c-Met inhibitor, suppresses the proliferation of lung cancer cells by downregulating the PI3K/AKT/mTOR and MAPK signaling pathways. Biochemical pharmacology. 2022, 195: 114864. 19. Yutang Huang,Yi Dai,Chunjie Wen,Shuai He,Jingjing Shi,Dezhang Zhao,Lanxiang Wu,Honghao Zhou circSETD3 Contributes to Acquired Resistance to Gefitinib in Non-Small-Cell Lung Cancer by Targeting the miR-520h/ABCG2 Pathway. Molecular Therapy-Nucleic Acids. 2020 20. Liang J, Bi G, Sui Q, et al.Transcription factor ZNF263 enhances EGFR-targeted therapeutic response and reduces residual disease in lung adenocarcinoma.Cell Reports.2024, 43(2). 21. Shao J, Ye Z, Shen Z, et al.Chidamide improves gefitinib treatment outcomes in NSCLC by attenuating recruitment and immunosuppressive function of myeloid-derived suppressor cells.Biomedicine & Pharmacotherapy.2024, 173: 116306.
收起
Ropsacitinib Cerdulatinib hydrochloride Delgocitinib Brepocitinib ST271 Lorlatinib NVP-BSK805 2HCl (1092499-93-8(free base)) Larotinib

相关化合物库

该产品包含在如下化合物库中:
抗癌临床化合物库 抗癌活性化合物库 酪氨酸激酶分子库 抗癌药物库 抗癌上市药物库 JAK-STAT 化合物库 高通量筛选天然产物库 天然产物库 血管生成库 抑制剂库

剂量换算

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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: 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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步: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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技术支持

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。

Keywords

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

 

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