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GDC-0449 (Vismodegib) is a potent and specific hedgehog (Hh) pathway, also inhibits ABCG2, Pgp and MRP1-important ABC transporters associated with MDR. The IC50 values of GDC-0449 for inhibition of ABCG2 and Pgp were 1.4 and 3.0μM, respectively. GDC-0449 (Vismodegib) has been used to treat medulloblastoma in animal models and has recently entered clinical trials for a variety of solid tumors.
Nature. 2020 Dec;588(7839):664-669.
Creation of bladder assembloids mimicking tissue regeneration and cancer
GDC-0449 (Vismodegib) purchased from AbMole
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Source | Pharma Res (2017). Figure 7. GDC-0449 |
| Method | i.v. | |
| Cell Lines | mice | |
| Concentrations | 10 mg/kg | |
| Incubation Time | 15, 30, 60, 240, 720 and 1440 min | |
| Results | For the 20% M6P-conjugated micelles, GDC-0449 concentration increased by 30.60% compared to non targeted micelles in normal mice and by 50.36% in fibrotic mice liver |
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Source | Pharma Res (2017). Figure 6. GDC-0449 |
| Method | i.v. | |
| Cell Lines | mice | |
| Concentrations | 10 mg/kg | |
| Incubation Time | 15, 30, 60, 240, 720 and 1440 min | |
| Results | Liver fibrosis results changes in the subendothelial space of Disse and sinusoid due to scar formation, which may affect the hepatic uptake of GDC-0449. The hepatic uptake of GDC-0449 after systemic administration of drug loaded micelles decreased from ~40% to ~30% |
| Cell Experiment | |
|---|---|
| Cell lines | OM9;22 cell line |
| Preparation method | Cell proliferation assay The cells were seeded in 24- or 96-well plates at a density of 2 *105 mL -1 in the presence or absence of S9 feeder cells. The cells were treated with the inhibitor drugs at the indicated concentrations: dasatinib, 1–100nM; and GDC-0449, 100nM to 10 mM. Viable cells were counted by trypan blue exclusion or fluorescence-activated cell sorting. |
| Concentrations | 100nM to 10 µM |
| Incubation time | 48h |
| Animal Experiment | |
|---|---|
| Animal models | Medulloblastoma allografts model in mice |
| Formulation | 0.5% methyl-cellulose, 0.2% tween-80 (MCT) |
| Dosages | 0.3 to 75 mg/kg daily |
| Administration | oral gavage |
| Molecular Weight | 421.3 |
| Formula | C19H14Cl2N2O3S |
| CAS Number | 879085-55-9 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Keating GM. Drugs. Vismodegib: in locally advanced or metastatic Basal cell carcinoma.
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All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
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