1. Stem Cell/Wnt Autophagy
  2. Hedgehog Autophagy
  3. Vismodegib

Vismodegib  (Synonyms: 维莫德吉; GDC-0449)

目录号: HY-10440 纯度: 99.95%
COA 产品使用指南

Vismodegib (GDC-0449) 是一种具有口服活性的 hedgehog 抑制剂,IC50 值为 3 nM;还可抑制 P-gpABCG2 的活性,IC50 值分别为 3.0 μM 和 1.4 μM。

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Vismodegib Chemical Structure

Vismodegib Chemical Structure

CAS No. : 879085-55-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥770
In-stock
5 mg ¥700
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10 mg ¥1080
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50 mg ¥2727
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100 mg ¥3972
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200 mg ¥5000
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1 g   询价  

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Customer Review

MCE 顾客使用本产品发表的 31 篇科研文献

WB
IF

    Vismodegib purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 28;420:195-207.  [Abstract]

    Shh-Light 2 cells are transfected with Gli1 or Gli2 plasmids and the expression of proteins are analyzed by Western blot. Positive control JQ1, CBC and CBD inhibit Gli1 and Gli2 overexpression induced Gli luciferase activity, GDC-0499 and GANT61 have no effects.

    Vismodegib purchased from MCE. Usage Cited in: Oncogenesis. 2018 Mar 13;7(3):24.  [Abstract]

    786-O and ACHN tumorspheres are treated with 0.1% CSE with/without 10 mM Vismodegib for 5 days. Western blotting analysis of SHH pathway proteins.

    Vismodegib purchased from MCE. Usage Cited in: J Genet Genomics. 2018 May 20;45(5):237-246.  [Abstract]

    Drug-feeding scheme (upper panel). Memory rescuing effects through treatment with LDE225 (LDE) or Vismodegib (VIS) at 20 mg/kg for 7.5-m-old and 15-m-old mice (lower panel, n=7 for each group).

    Vismodegib purchased from MCE. Usage Cited in: Anticancer Drugs. 2018 Mar;29(3):208-215.  [Abstract]

    SUM159 sphereforming cells are treated with 15 μM XAV-939 for 7 days, and the protein expression levels of breast cancer stem cells (CSCs) markers are detected by western blotting.

    Vismodegib purchased from MCE. Usage Cited in: Anticancer Drugs. 2018 Mar;29(3):208-215.  [Abstract]

    SUM159 sphere-forming cells are treated with Vismodegib (15 μM), a Smoothened (Smo) inhibitor for 7 days, and the protein expression levels of breast cancer stem cells (CSCs) play markers are detected by western blotting.

    Vismodegib purchased from MCE. Usage Cited in: Dev Neurobiol. 2017 Dec;77(12):1385-1400.  [Abstract]

    Reducing Shh signaling through Vismodegib treatment in Xenopus results in a significant rostral expansion of hypaxial muscle fibers.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively[1][2].

    IC50 & Target

    IC50: 3 nM (hedgehog), 3.0 μM (P-gp), 1.4 μM (ABCG2)[1][2]

    体外研究
    (In Vitro)

    Vismodegib (HhAntag691) 是一种 ABCG2 抑制剂,可通过阻断 HEK293 细胞中 NSC 279836 (另一种 ABCG2 底物) 的输出来增加其有效细胞内浓度。Vismodegib (HhAntag691,10 μM),使 MDCKII/Pgp 细胞和 MDCKII/MRP1 细胞对 NSC757 处理重新敏感[2]
    Vismodegib (25 μM 或 50 μM) 浓度依赖性地抑制 HCC 和 H1339 细胞[3]

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

    体内研究
    (In Vivo)

    Vismodegib (0.3 to 75 mg/kg,po) 在髓母细胞瘤同种异体移植肿瘤中非常有效。Vismodegib (> 46 mg/kg,口服) 导致患者来源的结直肠异种移植物生长延迟[4]

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

    Clinical Trial
    分子量

    421.30

    Formula

    C19H14Cl2N2O3S

    CAS 号
    性状

    固体

    颜色

    Off-white to light yellow

    中文名称

    维莫德吉

    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 1 year
    -20°C 6 months
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 50 mg/mL (118.68 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)

    Ethanol 中的溶解度 : 3.33 mg/mL (7.90 mM; 超声助溶 (<60°C))

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.3736 mL 11.8681 mL 23.7362 mL
    5 mM 0.4747 mL 2.3736 mL 4.7472 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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    • 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。

      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); 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。
    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: 99.97%

    参考文献
    Cell Assay
    [2]

    When MTT assay is performed, an MTT reagent is added to each well to a final concentration of 150 µg/mL, and the cells are incubated for 1 to 2 hours at 37°C. The medium is then replaced with DMSO to dissolve the reaction product. Absorbance at 570 nm is quantified using a spectra MAX 340pc plate reader. For the XTT assay, 1 mg/mL XTT is mixed with 0.025 mM PMS, and 50 µL of the mixture is added to each well and incubated for 4 hours at 37°C. After the plates are mixed on a plate shaker, absorbance at 450 nm is measured. All results are normalized to a percentage of absorbance obtained in controls.

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

    Animal Administration
    [2]

    Tumor-bearing mice are distributed into tumor volume-matched cohorts when the tumors reache between 200 and 350 mm3. The vismodegib-resistant medulloblastoma allograft, sg274, is developed by intermittent suboptimal dosing of a Ptch+/−, p53−/−medulloblastoma allograft. Vismodegib is formulated as a suspension in 0.5% methyl-cellulose, 0.2% tween-80 (MCT), and is administered orally. Tumor volumes are determined using digital calipers using the formula (L×W×W)/2. Tumor growth inhibition (%TGI) is calculated as the percentage of the area under the fitted curve (AUC) for the respective dose group per day in relation to the vehicle, such that %TGI=100×1-(AUCtreatment/day)/(AUCvehicle/day).

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

    参考文献

    Vismodegib 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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    Ethanol / DMSO 1 mM 2.3736 mL 11.8681 mL 23.7362 mL 59.3406 mL
    5 mM 0.4747 mL 2.3736 mL 4.7472 mL 11.8681 mL
    DMSO 10 mM 0.2374 mL 1.1868 mL 2.3736 mL 5.9341 mL
    15 mM 0.1582 mL 0.7912 mL 1.5824 mL 3.9560 mL
    20 mM 0.1187 mL 0.5934 mL 1.1868 mL 2.9670 mL
    25 mM 0.0949 mL 0.4747 mL 0.9494 mL 2.3736 mL
    30 mM 0.0791 mL 0.3956 mL 0.7912 mL 1.9780 mL
    40 mM 0.0593 mL 0.2967 mL 0.5934 mL 1.4835 mL
    50 mM 0.0475 mL 0.2374 mL 0.4747 mL 1.1868 mL
    60 mM 0.0396 mL 0.1978 mL 0.3956 mL 0.9890 mL
    80 mM 0.0297 mL 0.1484 mL 0.2967 mL 0.7418 mL
    100 mM 0.0237 mL 0.1187 mL 0.2374 mL 0.5934 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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