1. Stem Cell/Wnt
    Autophagy
  2. Hedgehog
    Autophagy

Vismodegib (Synonyms: GDC-0449)

Cat. No.: HY-10440 Purity: 99.91%
Data Sheet SDS 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

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
10 mg USD 60 In-stock
50 mg USD 78 In-stock
100 mg USD 101 In-stock
200 mg USD 132 In-stock
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Customer Review

  • 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
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References
Preparing Stock Solutions
Concentration Volume 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.
Cell Assay
[2]

Vismodegib is dissolved in DMSO.

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]

Vismodegib is formulated as a suspension in 0.5% methyl-cellulose, 0.2% tween-80 (MCT).

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

Purity: 99.91%

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Vismodegib
Cat. No.:
HY-10440
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