规格

价格

库存

数量

1 mg

¥ 378

现货

2 mg

¥ 546

现货

5 mg

¥ 897

现货

10 mg

¥ 1,530

现货

25 mg

¥ 2,620

现货

50 mg

¥ 3,890

现货

100 mg

¥ 5,690

现货

500 mg

¥ 11,700

现货

1 mL x 10 mM (in DMSO)

¥ 839

现货

生物活性

产品描述	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.
靶点活性	IGF-1R:35 nM, Insulin Receptor:75 nM, IRR:75 nM
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]
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.
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)
别名	林西替尼, OSI-906

化学信息

分子量	421.49
分子式	C₂₆H₂₃N₅O
CAS No.	867160-71-2
Smiles	NC=1C=2N(C(=NC2C3=CC4=C(C=C3)C=CC(=N4)C5=CC=CC=C5)[C@H]6C[C@@](C)(O)C6)C=CN1
密度	1.39 g/cm3

储存&溶解度

存储

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.

实际储存温度请以COA为准

溶解度信息

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 96 mg/mL (227.76 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.83 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3725 mL	11.8627 mL	23.7254 mL	118.6268 mL
5 mM	0.4745 mL	2.3725 mL	4.7451 mL	23.7254 mL
10 mM	0.2373 mL	1.1863 mL	2.3725 mL	11.8627 mL
20 mM	0.1186 mL	0.5931 mL	1.1863 mL	5.9313 mL
50 mM	0.0475 mL	0.2373 mL	0.4745 mL	2.3725 mL
100 mM	0.0237 mL	0.1186 mL	0.2373 mL	1.1863 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

Linsitinib

Linsitinib

产品介绍

引用文献

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剂量转换

关键词

Linsitinib

Linsitinib

Linsitinib 相关产品

产品介绍

引用文献

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剂量转换

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