1. Stem Cell/Wnt
  2. Porcupine
  3. LGK974

LGK974  (Synonyms: WNT974)

目录号: HY-17545 纯度: 99.92%
COA 产品使用指南

LGK974 (WNT974) 是一种有效的,具有口服活性的特异性 Porcupine (PORCN) 抑制剂,IC50 为 0.1 nM。

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LGK974 Chemical Structure

LGK974 Chemical Structure

CAS No. : 1243244-14-5

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1134
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2 mg ¥800
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5 mg ¥1300
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10 mg ¥2200
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50 mg ¥6500
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200 mg   询价  

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Top Publications Citing Use of Products

    LGK974 purchased from MCE. Usage Cited in: Cell Stem Cell. 2020 Sep 3;27(3):413-429.e4.  [Abstract]

    IF images of uninjured, 48 hpi, and 72 hpi mouse airway epithelia wild-type mice treated with vehicle or LGK974 assessing BrdU incorporation. Relative to vehicle-treated mice, LGK974-treated mice exhibited an attenuated SAE with few BrdU+ ABSCs, thereby phenocopying the repair response of K5-CreER;Ctnnb1fl/fl mouse tracheas.

    LGK974 purchased from MCE. Usage Cited in: Exp Cell Res. 2016 Jul 15;345(2):206-17.  [Abstract]

    Inhibition of PORCN abolishes Runx2 induction stimulated by β-GP. VSMCs are pretreated with LGK974 (1nM) for 30 min, then incubated with β-GP (10mM) for 24h, and the cell lysates are immunoblotted with antibodies against Runx2 and β-actin, respectively.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    LGK974 (WNT974) is an orally bioavailable and specific Porcupine (PORCN) inhibitor with an IC50 of 0.1 nM[1].

    IC50 & Target

    Porcupine[1]

    体外研究
    (In Vitro)

    在 PORCN 放射性配体结合试验中,LGK974 有效取代[3H]-GNF-1331,IC50 为 1 nM。LGK974 有效降低 HN30 细胞中 Wnt 依赖性 AXIN2 mRNA 水平,IC50 为 0.3 nM[1]

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

    体内研究
    (In Vivo)

    LGK974,一种靶向 Porcupine 的药物,Porcupine 是一种 Wnt 特异性酰基转移酶。LGK974 有效抑制 Wnt 信号,在啮齿动物肿瘤模型中具有强大的疗效,并且耐受性良好。在 3 和 20 mg/kg 的非荷瘤大鼠上进行毒理学研究。在每天 3 mg/kg 的有效剂量下,持续 14 天,LGK974 耐受性良好,在 Wnt 依赖性组织 (包括肠、胃和皮肤) 中没有异常组织病理学发现。当大鼠以每天 20 mg/kg 的极高剂量给药 14 天时,观察到肠上皮细胞丢失,这与 Wnt 是肠组织稳态所必需的概念一致[1]

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

    Clinical Trial
    分子量

    396.44

    Formula

    C23H20N6O

    CAS 号
    性状

    固体

    颜色

    White to light brown

    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
    In Vitro: 

    DMSO 中的溶解度 : ≥ 32 mg/mL (80.72 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.5224 mL 12.6122 mL 25.2245 mL
    5 mM 0.5045 mL 2.5224 mL 5.0449 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

    In Vivo:

    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    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (6.31 mM); 悬浊液; 超声加热助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      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。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.31 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,此方案实验周期在半个月以上的动物实验酌情使用。

      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玉米油中,混合均匀。

    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

    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: 99.92%

    参考文献
    Cell Assay
    [1]

    HN30 cells and UMSCC cells are used. For TaqMan assay, 2×106 cells per well are plated into six-well cell culture plates and treated with or without LGK974 in amultipoint dose-response. RNA samples are collected after 48 h. For colony formation assays, 2×103 cells per well are plated into six-well cell culture plates with or without compound treatment. Cells are stained with crystal violet 1 wk later[1].

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

    Animal Administration
    [1]

    Mice and Rats[1]
    Nude mice (or nude rats) bearing the mouse mammary tumor virus-Wnt1, HN30, or SNU1076 tumors are randomized according to tumor volume. LGK974 is formulated in 10% (vol/vol) citrate buffer (pH 2.8)/90% (vol/vol) citrate buffer (pH 3.0) or 0.5% MC/0.5% Tween 80 and administered by oral gavage at a dosing volume of 10 μL/g animal body weight. Body weight is monitored daily, and tumor sizes are assessed three times per week after the tumors are palpable. Tumor sizes are determined by using caliper measurements. Tumor volumes are calculated with a formula (length×width×height)/2. The plasma concentrations and exposures of LGK974 in the tumor-bearing nude mice (n=2 per dosing group) are determined on day 14. Blood samples (50 μL) are collected by serial retroorbital sampling at 1, 3, 7, 16, and 24 h postdose. The blood samples are centrifuged, and plasma is separated and frozen until analysis by liquid chromatography/MS/MS. For tolerability studies, LGK974 is administrated to nontumor-bearing Wistar rats one time per day by oral gavage at 3 or 20 mg/kg per day. Necropsies are performed at the end of the study. Tissues are fixed in 10% (vol/vol) neutralbuffered formalin, sectioned, and subjected to H&E staining.

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

    参考文献

    LGK974 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 2.5224 mL 12.6122 mL 25.2245 mL 63.0612 mL
    5 mM 0.5045 mL 2.5224 mL 5.0449 mL 12.6122 mL
    10 mM 0.2522 mL 1.2612 mL 2.5224 mL 6.3061 mL
    15 mM 0.1682 mL 0.8408 mL 1.6816 mL 4.2041 mL
    20 mM 0.1261 mL 0.6306 mL 1.2612 mL 3.1531 mL
    25 mM 0.1009 mL 0.5045 mL 1.0090 mL 2.5224 mL
    30 mM 0.0841 mL 0.4204 mL 0.8408 mL 2.1020 mL
    40 mM 0.0631 mL 0.3153 mL 0.6306 mL 1.5765 mL
    50 mM 0.0504 mL 0.2522 mL 0.5045 mL 1.2612 mL
    60 mM 0.0420 mL 0.2102 mL 0.4204 mL 1.0510 mL
    80 mM 0.0315 mL 0.1577 mL 0.3153 mL 0.7883 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.

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    目录号:
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