阿法替尼|T2303

價格	￥143	￥378
包裝	100mg	500mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:阿法替尼	英文名稱:(S)-Afatinib
CAS:439081-18-2	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: 99.96%	產(chǎn)品類別: 抑制劑
貨號: T2303

Product Introduction

Bioactivity

名稱	(S)-Afatinib
描述	(S)-Afatinib (BIBW2992) is an irreversible EGFR family inhibitor with IC50s of 0.5/0.4/10/14/1 nM for EGFRwt, EGFR (L858R), EGFR (L858R/T790M), HER2, and HER4, respectively.
細胞實驗	Cells (1×10^4) were transferred into each well of a 96-well plate and cultured over night in serum-free media for EGFR phosphorylation assay. After addition of test compounds on the next day, the plates were then incubated at 37°C for 1 hour. EGF-stimulation was done at 100 ng/ml for 10 min at room temperature. Cells were washed with ice cold PBS before extraction with 120 μl per well HEPEX buffer and shaken for 1 h at room temperature. In all 2×10^4 cells per well was used for HER2 phosphorylation assay. Streptavidin precoated plates were coated with anti-EGFR-biotin at 1:100 dilution with blocking buffer and c-erb2/HER2 oncoprotein Ab-5(Clone N24)-Biotin. Extracts from above steps were then transferred to the antibody-coated wells and incubated for 1 h at room temperature. Assessment of color development is described in Supplementary information. Extinction was measured at 450 nm. The data generated were analysed by the program PRISM. Normalized values were used to calculate the IC50 by a nonlinear regression curve fit (variable slope) [1].
激酶實驗	The wild type tyrosine kinase domain of the human EGFR, as well as the EGFR L858R/T790M double mutant, were fused to Glutathione-S-transferase (GST) and extracted as described in Supplementary methods. The L858R mutant was purchased from Upstate. Enzyme activity was then assayed in the presence or absence of serial inhibitor dilutions performed in 50% Me2SO. A random polymer pEY (4:1) from Sigma was used as substrate. Biotinylated pEY was added as a tracer substrate. The kinase domain of HER2 was cloned using baculovirus system and extracted similarly to that of EGFR kinase domain. Detailed procedures for EGFR, HER2, SRC, BIRK and VEGFR2 kinase activity assays are included in Supplementary information [1].
動物實驗	Six weeks old female athymic nude mice (nu/nu) weighing about 16-20 gram were housed by Laboratory Animal Services Centre of The Chinese University of Hong Kong. The experiment was conducted by researchers under license from the Hong Kong Government Department of Health and according to approval given by Animal Experimentation Ethics Committee of the Chinese University of Hong Kong. ESCC xenografts were established by inoculating HKESC-2 (0.6 × 10^5 cells re-suspended in 50 μl of HBSS-buffer) subcutaneously into both flanks of the nude mice. When tumor size reached to 4-6 mm diameter, they were randomized in either treatment (15 mg/kg) or vehicle control group. Afatinib for treatment was prepared by dissolving in 0.5% methylcellulose before administration. Either drug or vehicle was administered to mouse by oral gavage in a schedule of 5 days on plus 2 days off for two weeks. Drug efficacy was evaluated by monitoring the change in tumor size with caliper. Tumor volume was calculated with the formula Tumor Volume = (width2 × length)/2 [2].
體外活性	(S)-Afatinib對EGFR與HER2的野生型及其突變形式展示出強大活性（IC50分別為：EGFRwt 0.5 nM、EGFR L858R 0.4 nM、EGFR L858R/T790M 10 nM、HER2 14 nM）。在人類乳腺癌細胞系中，使用100 nM (S)-Afatinib足以阻止hereregulin刺激的HER3磷酸化作用[1]。食管鱗狀細胞癌（ESCC）細胞系對于afatinib敏感，IC50濃度處于較低μM范圍內(nèi)（72小時培養(yǎng)下：HKESC-1 = 0.002 μM、HKESC-2 = 0.002 μM、KYSE510 = 1.090 μM、SLMT-1 = 1.161 μM與EC-1 = 0.109 μM）。ErbB家族下游效應(yīng)物如pAKT、pS6與pMAPK的磷酸化在HKESC-2與EC-1中被顯著抑制。兩個細胞系在暴露于afatinib后24小時觀察到凋亡現(xiàn)象[2]。
體內(nèi)活性	每日口服BIBW2992，劑量為20 mg/kg，連續(xù)25天治療，顯著促進腫瘤退化并下調(diào)EGFR和AKT的磷酸化水平。通過NCIH1975細胞系（表達EGFR L858R/T790M）引起的異種移植瘤形成，經(jīng)BIBW2992處理后被有效控制，20 mg/kg劑量的T/C值為12% [1]。Afatinib能有效抑制小鼠體內(nèi)HKESC-2腫瘤生長，且無明顯毒副作用；單獨使用Afatinib在體內(nèi)模型中對食管鱗狀細胞癌（ESCC）表現(xiàn)出優(yōu)秀的生長抑制效果 [2]。
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 90 mg/mL (185.2 mM) Ethanol : 12 mg/mL (24.7 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 9 mg/mL (18.52 mM), Suspension. 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.
關(guān)鍵字	BIBW 2992 \| Afatinib \| BIBW-2992
相關(guān)產(chǎn)品	Lapatinib \| Neratinib \| Chalcone \| Gefitinib \| Erlotinib \| Osimertinib \| Erlotinib hydrochloride \| Afatinib Dimaleate \| Lidocaine Hydrochloride hydrate \| Genistein \| Khellin \| Osimertinib mesylate
相關(guān)庫	經(jīng)典已知活性庫 \| 已知活性化合物庫 \| 自噬庫 \| 抗結(jié)直腸癌化合物庫 \| 激酶抑制劑庫 \| FDA 上市藥物庫 \| FDA 上市激酶抑制劑庫 \| 酪氨酸激酶分子庫 \| 兒童藥物庫 \| 人代謝物化合物庫

關(guān)鍵字：阿法替尼|||BIBW2992|||(S)-阿法替尼|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。從虛擬篩選到實體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個性化定制合成；從對明確靶點的分子篩選到對明確分子的多靶點篩選，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	年營業(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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