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: 99.80%
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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10 mM * 1 mL in DMSO ¥770
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5 mg ¥700
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10 mg ¥1080
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200 mg ¥5000
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Top Publications Citing Use of Products

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

    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: Cancer Lett. 2018 Apr 28;420:195-207.

    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: Dev Neurobiol. 2017 Dec;77(12):1385-1400.

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

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

    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.

    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.

    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.
    • 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) is an ABCG2 inhibitor and can increase the effective intracellular concentration of NSC 279836, another ABCG2 substrate, through blocking its export in HEK293 cells. Vismodegib (HhAntag691, 10 µM), resensitizes MDCKII/Pgp cells and MDCKII/MRP1 cells to NSC757 treatment[2]. Vismodegib (25 μM or 50 μM) concentration dependently inhibits HCC and H1339 cells[3].

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

    体内研究
    (In Vivo)

    Vismodegib is a novel small molecule HPI, often used for clinical trials[1]. Vismodegib (0.3 to 75 mg/kg, p.o.) is highly efficacious in medulloblastoma allograft tumors. Vismodegib (> 46 mg/kg, p.o.) causes growth delay in patient-derived colorectal xenografts[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
    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 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 50 mg/mL (118.68 mM; Need ultrasonic)

    Ethanol : 3.33 mg/mL (7.90 mM; ultrasonic and warming and heat to 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 11.8680 mL 23.7361 mL
    5 mM 0.4747 mL 2.3736 mL 4.7472 mL
    10 mM 0.2374 mL 1.1868 mL 2.3736 mL
    *

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

    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

    • 1.

      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); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.93 mM,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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 2.

      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); Suspended solution; Need ultrasonic and warming

      此方案可获得 2.5 mg/mL (5.93 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      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。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    • 3.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.93 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (5.93 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      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玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    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

    纯度: 99.97%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    目录号:
    HY-10440
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