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

Vismodegib  (Synonyms: GDC-0449)

製品番号: HY-10440 純度: 99.95%
COA 取扱説明書

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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.

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Vismodegib 構造式

Vismodegib 構造式

CAS 番号 : 879085-55-9

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無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 在庫あり
Solution
10 mM * 1 mL in DMSO USD 73 在庫あり
Solid
10 mg USD 66 在庫あり
50 mg USD 86 在庫あり
100 mg USD 111 在庫あり
200 mg USD 145 在庫あり
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カスタマーレビュー

Based on 37 publication(s) in Google Scholar

Vismodegib 関連抗体

Top Publications Citing Use of Products

顧客検証

WB
IF

    Vismodegib purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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.

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    製品説明

    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]
    体外実験

    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].

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

    Vismodegib 関連抗体
    体内実験

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    421.30

    分子式

    C19H14Cl2N2O3S
    CAS 番号
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(C1=CC=C(C=C1Cl)S(=O)(C)=O)NC2=CC=C(C(C3=NC=CC=C3)=C2)Cl
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 50 mg/mL (118.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 3.33 mg/mL (7.90 mM; ultrasonic and warming and heat to 60°C)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.2374 mL 1.1868 mL 2.3736 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

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

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.93 mM); Suspended solution; Need ultrasonic and warming

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.97%

    COA (249 KB) HNMR (218 KB) LCMS (139 KB) Elemental Analysis Report (107 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [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).

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 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
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    Vismodegib Related Classifications

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2
    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:

    Vismodegib879085-55-9GDC-0449GDC0449GDC 0449HedgehogAutophagyInhibitorinhibitorinhibit

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