吉非替尼|T1181

價(jià)格	￥798	￥460	￥327
包裝	500mg	100mg	50mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-14

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產(chǎn)品詳情

中文名稱:吉非替尼	英文名稱:Gefitinib
CAS:184475-35-2	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.92%	產(chǎn)品類別: 抑制劑
貨號: T1181

Product Introduction

Bioactivity

名稱	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.
細(xì)胞實(shí)驗(yàn)	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].
動(dòng)物實(shí)驗(yàn)	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].
體外活性	方法：23 種腫瘤細(xì)胞用 Gefitinib 處理 72 h，使用 MTT 方法檢測細(xì)胞活力。結(jié)果：只有 PC9 細(xì)胞系的 IC50<1 μmol/L (高度敏感)，14 個(gè)細(xì)胞系的 IC50>10 μmol/L (抗性)，其余 8 個(gè)細(xì)胞系具有 1-10 μmol/L 的 IC50 (中等敏感）。[1] 方法：腫瘤細(xì)胞 HT29、KB、Du145 和 A549 用 Gefitinib (0.032-50 μM) 處理 2 h，在細(xì)胞裂解前五分鐘加入 EGF (0.1 μg/mL)，使用 Western Blot 方法檢測靶點(diǎn)蛋白表達(dá)水平。結(jié)果：Gefitinib 在所有腫瘤細(xì)胞系中產(chǎn)生 EGFR 自磷酸化的劑量依賴性抑制。[2]
體內(nèi)活性	方法：為檢測體內(nèi)抗腫瘤活性，將 Gefitinib (3.125-200 mg/kg in 0.5% polysorbate 80) 口服給藥給攜帶腫瘤 A431、 Du145 或 A549 的 nude 小鼠，每天一次，持續(xù)七-十五天。結(jié)果：Gefitinib 劑量依賴性方式抑制 A431、 Du145 或 A549 腫瘤生長。[2] 方法：為檢測體內(nèi)抗腫瘤活性，將 Gefitinib (40 mg/kg，每天一次) 或 Gefitinib (200 mg/kg，每五天一次) 灌胃給藥給攜帶人肺癌腫瘤 H3255 的 athymic nude 小鼠，持續(xù)兩周。結(jié)果：每周治療顯示出比每天治療更好的抑制作用。與每日給藥方案相比，每周給藥方案對 p-EGFR、p-ERK 和 p-AKT 的抑制作用更強(qiáng)。[3]
存儲(chǔ)條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	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), Working solution is recommended to be prepared and used immediately.
關(guān)鍵字	EGFR tyrosine kinase \| Autophagy \| lung cancer \| breast cancer \| phosphorylation \| Inhibitor \| Apoptosis \| inhibit \| TAMs \| NSCLCs \| EGFR \| antitumour \| Epidermal growth factor receptor \| HER1 \| tumor metastasis \| Gefitinib \| ZD-1839 \| ZD 1839 \| ErbB-1
相關(guān)庫	抗癌活性化合物庫 \| 已知活性化合物庫 \| 生物堿類天然產(chǎn)物庫 \| EMA 上市藥物庫 \| 膜蛋白靶向化合物庫 \| 藥物功能重定位化合物庫 \| 抗癌臨床化合物庫 \| 抗癌藥物庫

關(guān)鍵字： ZD1839|||吉非替尼|TargetMol

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對明確靶點(diǎn)的分子篩選到對明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國市場五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊資本	566.2651萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊資本：566.2651萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑，藥物篩選化合物庫，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場三路28號4樓

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