尼洛替尼|T1524

價(jià)格	￥282	￥460	￥713
包裝	25mg	50mg	100mg

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:尼洛替尼	英文名稱:Nilotinib
CAS:641571-10-0	品牌: TargetMol
產(chǎn)地: 美國(guó)	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: 99.83%	產(chǎn)品類別: 抑制劑
貨號(hào): T1524

Product Introduction

Bioactivity

名稱	Nilotinib
描述	Nilotinib (AMN107) is a Bcr-Abl tyrosine kinase inhibitor with oral activity. Nilotinib has antitumor activity and may be used for the treatment of Imatinib-resistant chronic myelogenous leukemia (CML).
細(xì)胞實(shí)驗(yàn)	Ba/F3 cell lines were plated in triplicate and incubated with escalating concentrations of imatinib, AMN107, or BMS-354825 for 72 hours. Proliferation was measured using a methanethiosulfonate-based viability assay. IC50 and IC90 values are reported as the mean of three independent experiments done in quadruplicate. The inhibitor concentration ranges for IC50 and IC90 determinations were 0 to 2,000 nmol/L (imatinib and AMN107) or 0 to 32 nmol/L (BMS-354825). The imatinib concentration range was extended to 6,400 nmol/L for mutants with IC50 >2,000 nmol/L. The BMS-354825 concentration range was extended to 200 nmol/L for mutant T315I [1].
激酶實(shí)驗(yàn)	Kinase assays using wild-type and mutant glutathione S-transferase (GST)–Abl fusion proteins (c-Abl amino acids 220-498) were done as described, with minor alterations. GST-Abl fusion proteins were released from glutathione-Sepharose beads before use; the concentration of ATP was 5 μmol/L. Immediately before use in kinase autophosphorylation and in vitro peptide substrate phosphorylation assays, GST-Abl kinase domain fusion proteins were treated with LAR tyrosine phosphatase according to the manufacturer's instructions. After 1-hour incubation at 30°C, LAR phosphatase was inactivated by addition of sodium vanadate (1 mmol/L). Immunoblot analysis comparing untreated GST-Abl kinase to dephosphorylated GST-Abl kinase was routinely done using phosphotyrosine-specific antibody 4G10 to confirm complete (>95%) dephosphorylation of tyrosine residues and c-Abl antibody CST 2862 to confirm equal loading of GST-Abl kinase. The inhibitor concentration ranges for IC50 determinations were 0 to 5,000 nmol/L (imatinib and AMN107) or 0 to 32 nmol/L (BMS-354825). The BMS-354825 concentration range was extended to 1,000 nmol/L for mutant T315I. These same inhibitor concentrations were used for the in vitro peptide substrate phosphorylation assays. The three inhibitors were tested over these same concentration ranges against GST-Src kinase and GST-Lyn kinase [1].
動(dòng)物實(shí)驗(yàn)	The GIST xenograft lines GK1X, GK2X and GK3X in nude mice were established from GIST patients as described in our previous study [10]. These xenograft lines were maintained by continual passage in BALB/cSLc-nu/nu mice. Mice bearing GK1X, GK2X and GK3X tumors (6–8 mice per group) were treated daily with vehicle or 40 mg/kg imatinib or nilotinib for 4 weeks. Tumor volume (TV) was determined from caliper measurements of tumor length (L) and width (w) according to the formula LW2/2. TV was determined every two to three days and on the day of evaluation. Mice were sacrificed and the percentage of tumor growth inhibition (TGI) was calculated as follows: TGI (%) ?=? [1– (mean of treatment group tumor volume on evaluation day – mean of treatment group tumor volume on day 1)/(mean of control group tumor volume on evaluation day – mean of control group tumor volume on day 1)]×100 [2].
體外活性	方法: 表達(dá) Bcr-Abl 的野生型或突變體的 Ba/F3 細(xì)胞用 Nilotinib 處理 72 h，使用 methanethiosulfonate-based viability assay 檢測(cè)細(xì)胞活力。結(jié)果: Nilotinib 以比 imatinib 高 20 倍的效力抑制表達(dá)野生型 Bcr-Abl 的細(xì)胞的生長(zhǎng) (IC50:13 對(duì) 260 nmol/L)。除了T315I外，所有測(cè)試的 imatinib 抗性突變體都保持了類似的改善。[1] 方法: 黑色素瘤細(xì)胞系 D04 用 Nilotinib (0.1-10 μM) 處理 3 h，使用 Western Blot 方法檢測(cè)靶點(diǎn)蛋白表達(dá)水平。結(jié)果: Nilotinib 在低至 100 nM 的濃度下刺激了強(qiáng)大的 MEK 和 ERK 磷酸化。[2]
體內(nèi)活性	方法: 為檢測(cè)體內(nèi)抗腫瘤活性，將 Nilotinib (25 mg/kg) 和 PD184352 (25 mg/kg) 灌胃給藥給攜帶 BCR-ABL 或 BCR-ABLT315I 的 Ba/F3 同種異體移植物的 Balb/cJ 小鼠，每天一次，持續(xù)二十天。結(jié)果: Nilotinib 強(qiáng)烈抑制 BCR-ABL 腫瘤的生長(zhǎng)，但 PD184352 沒(méi)有抑制，PD184352 也沒(méi)有增強(qiáng) Nilotinib 的生長(zhǎng)抑制活性。相反，BCR-ABLT315I 腫瘤對(duì) Nilotinib 和 PD184352 都不敏感，但這些藥物協(xié)同作用抑制了腫瘤的生長(zhǎng)。[2]
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	H2O : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2.6 mg/mL (4.91 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. Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 13.75 mg/mL (25.97 mM)
關(guān)鍵字	Nilotinib \| antitumor \| AMN-107 \| AMN 107 \| tyrosine kinase \| Inhibitor \| Bcr-Abl \| Autophagy \| inhibit
相關(guān)產(chǎn)品	Guanidine hydrochloride \| Naringin \| Valproic Acid \| Taurine \| Gefitinib \| Aceglutamide \| Hydroxychloroquine \| Curcumin \| Stavudine \| Salicylic acid \| Paeonol \| Sodium 4-phenylbutyrate
相關(guān)庫(kù)	抑制劑庫(kù) \| 抗癌活性化合物庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| EMA 上市藥物庫(kù) \| 抗衰老化合物庫(kù) \| FDA 上市激酶抑制劑庫(kù) \| 藥物功能重定位化合物庫(kù) \| 抗癌臨床化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字：尼洛替尼|||尼羅替尼|||Tasigna|||AMN107|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)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(duì)明確靶點(diǎn)的分子篩選到對(duì)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(guò)在中國(guó)市場(chǎng)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(guò)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(cè)資本	566.2651萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

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公司成立：12年
注冊(cè)資本：566.2651萬(wàn)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(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫(kù)，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(chǎng)三路28號(hào)4樓

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