林西替尼|T6017

Linsitinib
867160-71-2

询价 1removed 起订

上海更新日期：2026-05-08

TargetMol中国（陶术生物）

VIP14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：: 林西替尼

英文名称：: Linsitinib

CAS号：: 867160-71-2

品牌：: TargetMol

产地：: 美国

保存条件：: 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.

纯度规格：: 99.92%

产品类别：: 抑制剂

货号：: T001|T6017

Product Introduction

Bioactivity

名称	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.
细胞实验	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)
激酶实验	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.
体外活性	方法：在SW48结肠癌细胞中，Linsitinib（1.0或10.0 μmol/L）预处理48小时，再以Regorafenib（5 μmol/L）处理96小时。结果：MTT法检测显示细胞存活率降至42±7%，表明Linsitinib可抑制Regorafenib耐药性。[1] 方法：在PC9、HCC827及H1975人肺癌细胞中，经Linsitinib（10 μmol/L）处理5天后，MTT法检测显示细胞增殖受抑。结果：联合Gefitinib可协同抑制PC9和HCC827细胞活力，并增加HCC827及H1975细胞凋亡率。Western blot证实其机制与抑制IGF-1R及下游AKT/ERK磷酸化相关。[2] 方法：在H295R和HAC15人肾上腺皮质癌细胞中，经Linsitinib处理3或6天后，DNA含量测定显示细胞增殖呈剂量和时间依赖性抑制. 方法：IC50值分别为1.5×10⁻⁷ M和2.9×10⁻⁸ M。同时，DNA片段化检测证实其可诱导细胞凋亡。[3]
体内活性	方法：在AOM/DSS诱导的C57BL/6J小鼠结肠癌模型中，Linsitinib与Regorafenib联合口服给药。结果：联合治疗显著抑制体重下降，减少肿瘤数量（最低1±1个），并延长生存期（40%）。[1]
存储条件	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.
关键字	OSI906 \| OSI 906 \| Linsitinib \| IRR \| Insulin Receptor \| Inhibitor \| inhibit \| IGF-1R \| IGF1R
相关产品	Urolithin C \| Tranexamic acid \| (2S,3R,4S)-4-Hydroxyisoleucine \| Semaglutide \| Sorbic acid \| Insulin (human) \| Picropodophyllin \| L-Cysteine hydrochloride hydrate \| Ornithine-α-ketoglutarate \| Brigatinib \| Morin \| Indirubin Derivative E804
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌活性化合物库 \| 已知活性化合物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| 膜蛋白靶向化合物库 \| 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 \| 人代谢物化合物库 \| 抗癌药物库

林西替尼;OSI-906;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	(14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