吉非替尼|T1181

Gefitinib
184475-35-2

￥798 500mg 起订

￥460 100mg 起订

￥327 50mg 起订

上海更新日期：2026-01-06

TargetMol中国（陶术生物）

VIP13年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 吉非替尼

英文名称：: Gefitinib

CAS号：: 184475-35-2

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

纯度规格：: 100.00%

产品类别：: 抑制剂

货号：: T1181

Product Introduction

Bioactivity

名称	Gefitinib
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.
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].
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]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
溶解度	DMSO : 18.33 mg/mL (41.02 mM), Sonication is recommended. Ethanol : 4.5 mg/mL (10.07 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4.47 mg/mL (10 mM), Solution.
关键字	ZD-1839 \| ZD 1839 \| TyrosineKinases \| Tyrosine Kinases \| Tyr992 (NR6wtEGFR cells) \| Tyr992 (NR6W cells) \| Tyr992 \| Tyr1173 (NR6wtEGFR cells) \| Tyr1173 (NR6W cells) \| tumor metastasis \| TAMs \| phosphorylation \| NSCLCs \| lung cancer \| Inhibitor \| inhibit \| HER1 \| Gefitinib \| ErbB-1 \| Epidermal growth factor receptor \| EGFR tyrosine kinase \| EGFR \| breast cancer \| Autophagy \| Apoptosis \| antitumour
相关产品	Urea \| Naringin \| Guanidine hydrochloride \| Aceglutamide \| Alginic acid \| Cysteamine hydrochloride \| Metronidazole \| Hemin \| Hydroxychloroquine \| Stavudine \| Tamoxifen \| Paeonol
相关库	抑制剂库 \| 已知活性化合物库 \| 植物来源化合物库 \| 生物碱类天然产物库 \| EMA 上市药物库 \| 抗衰老化合物库 \| FDA 上市药物库 \| 免疫/炎症分子化合物库 \| 酪氨酸激酶分子库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

吉非替尼|||ZD1839|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(13年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子