林西替尼|T6017

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價(jià)格	詢價(jià)
包裝	1removed

最小起訂量	1removed
發(fā)貨地	上海
更新日期	2026-05-08

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產(chǎn)品詳情

中文名稱:林西替尼	英文名稱:Linsitinib
CAS:867160-71-2	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Store at low temperature Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
純度規(guī)格: 99.92%	產(chǎn)品類別: 抑制劑
貨號(hào): T001\|T6017

Product Introduction

Bioactivity

名稱	Linsitinib
描述	Linsitinib (OSI-906) belongs to small molecule inhibitors and is a dual IGF-1/IR inhibitor (IC₅₀ = 35 and 75 nM, respectively) with selectivity, cell permeability, and oral activity. This compound is used in antitumor research and can effectively inhibit cell proliferation and induce apoptosis.
細(xì)胞實(shí)驗(yàn)	For assays of cell proliferation, cells are seeded into 96-well plates in appropriate media containing FCS 10% and incubated for 3 days in the presence of OSI-906 at various concentrations. Inhibition of cell growth is determined by luminescent quantitation of intracellular ATP content using CellTiterGlo. Data is presented as a fraction of maximal proliferation, calculated by dividing the cellular density in the presence of varying concentrations of OSI-906 by the cellular density of control cells treated with vehicle (DMSO) only.(Only for Reference)
激酶實(shí)驗(yàn)	Protein kinase biochemical assays: Protein kinase assays are either performed in-house by ELISA-based assay methods (IGF-1R,IR,EGFR and KDR) or at Upstate Inc.by a radiometric method with ATP at 100 μM concentration.In-house ELISA assays use poly(Glu:Tyr) as the substrate bound to the surface of 96-well assay plates and phosphorylation is detected using an antiphosphotyrosine antibody conjugated to horseradish peroxidase.The bound antibody is quantified using ABTS as the peroxidase substrate by measuring absorbance at 405 / 490 nm.All assays use purified recombinant kinase catalytic domains.Recombinant enzymes of human IGF-1R or EGFR are expressed as an NH2-terminal glutathione S-transferase fusion protein in insect cells and are purified in house.IC50 values are determined from the sigmoidal dose–response plot of percent inhibition versus log10 compound concentration.A minimum of three measurements,performed in duplicate,are carried out with in-house assays unless otherwise indicated.OSI-906 at a concentration of 1 μM is profiled versus a panel of kinases using the ProfilerProTM Kinase Selectivity Assay Kit.
體外活性	方法：在SW48結(jié)腸癌細(xì)胞中，Linsitinib（1.0或10.0 μmol/L）預(yù)處理48小時(shí)，再以Regorafenib（5 μmol/L）處理96小時(shí)。結(jié)果：MTT法檢測(cè)顯示細(xì)胞存活率降至42±7%，表明Linsitinib可抑制Regorafenib耐藥性。[1] 方法：在PC9、HCC827及H1975人肺癌細(xì)胞中，經(jīng)Linsitinib（10 μmol/L）處理5天后，MTT法檢測(cè)顯示細(xì)胞增殖受抑。結(jié)果：聯(lián)合Gefitinib可協(xié)同抑制PC9和HCC827細(xì)胞活力，并增加HCC827及H1975細(xì)胞凋亡率。Western blot證實(shí)其機(jī)制與抑制IGF-1R及下游AKT/ERK磷酸化相關(guān)。[2] 方法：在H295R和HAC15人腎上腺皮質(zhì)癌細(xì)胞中，經(jīng)Linsitinib處理3或6天后，DNA含量測(cè)定顯示細(xì)胞增殖呈劑量和時(shí)間依賴性抑制. 方法：IC50值分別為1.5×10?? M和2.9×10?? M。同時(shí)，DNA片段化檢測(cè)證實(shí)其可誘導(dǎo)細(xì)胞凋亡。[3]
體內(nèi)活性	方法：在AOM/DSS誘導(dǎo)的C57BL/6J小鼠結(jié)腸癌模型中，Linsitinib與Regorafenib聯(lián)合口服給藥。結(jié)果：聯(lián)合治療顯著抑制體重下降，減少腫瘤數(shù)量（最低1±1個(gè)），并延長(zhǎng)生存期（40%）。[1]
存儲(chǔ)條件	Store at low temperature Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.83 mM), Sonication is recommended. DMSO : 96 mg/mL (227.76 mM), Sonication is recommended.
關(guān)鍵字	OSI906 \| OSI 906 \| Linsitinib \| IRR \| Insulin Receptor \| Inhibitor \| inhibit \| IGF-1R \| IGF1R
相關(guān)產(chǎn)品	Urolithin C \| Tranexamic acid \| (2S,3R,4S)-4-Hydroxyisoleucine \| Sorbic acid \| Insulin (human) \| Picropodophyllin \| L-Cysteine hydrochloride hydrate \| Ornithine-α-ketoglutarate \| Brigatinib \| Morin \| Indirubin Derivative E804 \| BMS-754807
相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 抗癌活性化合物庫(kù) \| 已知活性化合物庫(kù) \| 靶向治療藥物庫(kù) \| 激酶抑制劑庫(kù) \| 抗衰老化合物庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 酪氨酸激酶分子庫(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：林西替尼;OSI-906;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 （14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)

TargetMol中國(guó)（陶術(shù)生物）

VIP 14年

公司成立：14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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