2. Protein Tyrosine Kinase/RTK
  3. IGF-1R Insulin Receptor
  4. Linsitinib

Linsitinib  (Synonyms: OSI-906)

目录号: HY-10191 纯度: 99.84%
COA 产品使用指南

摩尔计算器

Linsitinib (OSI-906) 是一种有效选择性的，具有口服活性的 IGF-1 和胰岛素受体 (IR) 的双重抑制剂，IC50 分别为 35 和 75 nM。

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Linsitinib Chemical Structure

Linsitinib Chemical Structure

CAS No. : 867160-71-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1020
In-stock
2 mg ￥683
In-stock
5 mg ￥1100
In-stock
10 mg ￥1850
In-stock
50 mg ￥4700
In-stock
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

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Customer Review

Linsitinib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 38 篇科研文献

WB

    Linsitinib purchased from MCE. Usage Cited in: Cell Metab. 2017 Apr 4;25(4):868-882.e5.  [Abstract]

    Western blot of indicated proteins in control β cells in the presence of 10 nM Insulin, 200 nM OSI-906 (IR/IGF1Ri), 50μM LY294002 (PI3Ki), 5μM MK-2206 (Akti), or 20μM U0126 (MEKi) for 24 hr. Bottom: intensity of the signals quantified by densitometry.

    Linsitinib purchased from MCE. Usage Cited in: Sci Rep. 2017 Jun 23;7(1):4119.  [Abstract]

    Transient hyperglycemia accompanied by ephemeral hyperinsulinemia induced by IR and IGF1R inhibition with OSI-906. C57BL/6J mice are subjected to a 16-hour fast and OSI-906 (45 mg/kg) or a vehicle (Solutol HS-15) is administered orally 1 hour before injection with either saline, 10 units of insulin, or 1 mg/kg of IGF-1 via the inferior vena cava. The liver and epididymal fat are collected 70 and 120 seconds after injection, respectively.

    Linsitinib purchased from MCE. Usage Cited in: BMC Cancer. 2017 Dec 5;17(1):820.  [Abstract]

    OSI-906 inhibits p-IGF1R and IGF1R signaling factors in breast cancer cell-lines. 3 × 105 ER-positive MCF7 and ER-negative are plated per well of a 6-well plate and cultured for 24 h and subsequently treated with the OSI-906 (0.1, 0.4 and 1.6 μM) and/or SKI-II (4 μM) for 24 h. Protein lysates are collected and 20 μg of protein is used for immunoblot analysis to measure changes to IGF1R signaling and SphK1 steady-state protein expression levels.

    Linsitinib purchased from MCE. Usage Cited in: BMC Cancer. 2017 Dec 5;17(1):820.  [Abstract]

    OSI-906 inhibits p-IGF1R and IGF1R signaling factors in breast cancer cell-lines. HCC-1806 breast cancer cells are plated per well of a 6-well plate and cultured for 24 h and subsequently treated with OSI-906 (0.1, 0.4 and 1.6 μM) and/or SKI-II (4 μM) for 24 h. Protein lysates are collected and 20 μg of protein is used for immunoblot analysis to measure changes to IGF1R signaling and SphK1 steady-state protein expression levels.

    Linsitinib purchased from MCE. Usage Cited in: Department of Dental Pharmacology. Okayama University. 2015.

    The role of Semaphorin4D in bone invasion by oral cancer.

    Linsitinib purchased from MCE. Usage Cited in: Endocrinology. 2014 Jun;155(6):2102-11.  [Abstract]

    OSI-906 inhibits insulin receptor-mediated signaling in HEK293 cells. The cells are deprived of serum for 2 hours, stimulated for 5 min with 1 μM i nsulin in the presence or absence of 200 nM OSI-906 in serum-free medium. Cell extracts are subjected to immunoprecipitation and immunoblotting, as indicated.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Linsitinib (OSI-906) is a potent, selective and orally bioavailable dual inhibitor of the IGF-1 receptor and insulin receptor (IR) with IC50s of 35 and 75 nM, respectively[1].

    IC50 & Target

    IC50: 35 nM (IGF-1R), 75 nM (InsR)[1]
    体外研究
    (In Vitro)

    Linsitinib 抑制 IGF-1R 自磷酸化和下游信号蛋白 Akt、ERK1/2 和 S6 激酶的激活，IC50 为 0.028 至 0.13 μM。Linsitinib 通过与 C 螺旋的相互作用使靶蛋白形成中间构象。Linsitinib 在肝微粒体中表现出良好的代谢稳定性。Linsitinib 在浓度为 1 μM 时完全抑制 IR 和 IGF-1R 磷酸化。Linsitinib 抑制多种肿瘤细胞系的增殖，包括非小细胞肺癌和结直肠癌 (CRC) 肿瘤细胞系，EC50 为 0.021 至 0.810 μM[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Linsitinib 相关抗体:
    体内研究
    (In Vivo)

    Linsitinib 在 IGF-1R 驱动的异种移植小鼠模型中抑制肿瘤生长，在 75 mg/kg 剂量下有 100% TGI 和 55% 消退，在 25 mg/kg 剂量下有 60% TGI 无消退。Linsitinib 给药在狗、大鼠和小鼠中诱导不同的自身消除半衰期，消除半衰期分别为1.18小时、2.64小时和2.14小时。Linsitinib 在雌性 Sprague-Dawley 大鼠和雌性 CD-1 小鼠中以不同的单剂量每天一次给药表明 Vmax 与 Linsitinib 剂量不成比例。Linsitinib 在给药 12 天后以 25 mg/kg 的剂量升高血糖水平。在 IGF-1R 驱动的全长人 IGF-1R (LISN) 异种移植小鼠模型中以 75 mg/kg 的单剂量给予 Linsitinib，在 4 至 24 小时内使用血浆药物实现对 IGF-1R 磷酸化的最大抑制 (80%) 浓度为 26.6-4.77 μM[1]。在 NCI-H292 异种移植小鼠中以 60 mg/kg 的单剂量给药 Linsitinib 在体内处理后 2、4 和 24 小时抑制葡萄糖摄取。Linsitinib 在 NCI-H292 异种移植小鼠模型中抑制肿瘤的生长[2]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    421.49

    Formula

    C26H23N5O
    CAS 号
    性状

    固体

    颜色

    White to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 50 mg/mL (118.63 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.3725 mL 11.8627 mL 23.7254 mL
    5 mM 0.4745 mL 2.3725 mL 4.7451 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.93 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.93 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： 30% Solutol HS-15 in Saline

      Solubility: 5 mg/mL (11.86 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.84%

    COA (292 KB) LCMS (103 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    Protein kinase assays are either performed in-house by ELISA-based assay methods (IGF-1R, IR, EGFR and KDR) or 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. Linsitinib at a concentration of 1 µM is profiled versus a panel of kinases using the ProfilerProTM Kinase Selectivity Assay Kit.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    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 Linsitinib 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 Linsitinib by the cellular density of control cells treated with vehicle (DMSO) only.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Cells are harvested from cell culture flasks during exponential cell growth, washed twice with sterile PBS to a suitable concentration before subcutaneous implantation on the right flank of female nu/nu CD-1 mice. Tumors are established to 200±50 mm3 in size before randomization into treatment groups of eight mice each for efficacy studies. Linsitinib or vehicle is administered orally as indicated. The %TGI values indicated are the median %TGI over the entire dosing period. TGI of at lease 505 is considered significant. Growth delay is calculated as T-C shere T and C are the times in days for mean tumor size in the treated (T) and control (C) groups to reach 400% of the initial tumor volume. Cures are excluded from this calculation.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Linsitinib 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3725 mL 11.8627 mL 23.7254 mL 59.3134 mL
    5 mM 0.4745 mL 2.3725 mL 4.7451 mL 11.8627 mL
    10 mM 0.2373 mL 1.1863 mL 2.3725 mL 5.9313 mL
    15 mM 0.1582 mL 0.7908 mL 1.5817 mL 3.9542 mL
    20 mM 0.1186 mL 0.5931 mL 1.1863 mL 2.9657 mL
    25 mM 0.0949 mL 0.4745 mL 0.9490 mL 2.3725 mL
    30 mM 0.0791 mL 0.3954 mL 0.7908 mL 1.9771 mL
    40 mM 0.0593 mL 0.2966 mL 0.5931 mL 1.4828 mL
    50 mM 0.0475 mL 0.2373 mL 0.4745 mL 1.1863 mL
    60 mM 0.0395 mL 0.1977 mL 0.3954 mL 0.9886 mL
    80 mM 0.0297 mL 0.1483 mL 0.2966 mL 0.7414 mL
    100 mM 0.0237 mL 0.1186 mL 0.2373 mL 0.5931 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Linsitinib867160-71-2OSI-906OSI906OSI 906IGF-1RInsulin ReceptorInsulin-like growth factor-1 receptorInhibitorinhibitorinhibit

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