1. Stem Cell/Wnt
    Autophagy
  2. Hedgehog
    Autophagy

Vismodegib (Synonyms: GDC-0449)

Cat. No.: HY-10440 Purity: 99.91%
Handling Instructions

Vismodegib is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM and also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively.

For research use only. We do not sell to patients.

Vismodegib Chemical Structure

Vismodegib Chemical Structure

CAS No. : 879085-55-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 78 In-stock
Estimated Time of Arrival: December 31
100 mg USD 101 In-stock
Estimated Time of Arrival: December 31
200 mg USD 132 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Customer Review

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Vismodegib is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM and also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively.

    IC50 & Target

    IC50: 3 nM (hedgehog), 3.0 μM (P-gp), 1.4 μM (ABCG2)

    In Vitro

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

    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].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (118.68 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

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

    • 2.

      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

    • 3.

      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

    References
    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.

    References
    Molecular Weight

    421.30

    Formula

    C₁₉H₁₄Cl₂N₂O₃S

    CAS No.

    879085-55-9

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.91%

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    Product Name:
    Vismodegib
    Cat. No.:
    HY-10440
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    Vismodegib

    Cat. No.: HY-10440