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GDC-0449

Cat. No. M1713
GDC-0449 Structure
Synonym:

Vismodegib, HhAntag691

Size Price Availability Quantity
10mg USD 60 In stock
50mg USD 80 In stock
200mg USD 130 In stock
1g USD 460 In stock
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Quality Control
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 421.3
Formula C19H14Cl2N2O3S
CAS Number 879085-55-9
Purity 98.70%
Solubility DMSO
Storage at -20°C
References

Initial Assessment of Tumor Regrowth After Vismodegib in Advanced Basal Cell Carcinoma.
Chang et al. Arch Dermatol. 2012 Aug 20;1-2. PMID: 22910979.

Vismodegib: a promising drug in the treatment of basal cell carcinomas.
Dirix et al. Future Oncol. 2012 Aug;8(8):915-28. PMID: 22894666.

Vismodegib: in locally advanced or metastatic Basal cell carcinoma.
Keating GM. Drugs. 2012 Jul 30;72(11):1535-41. PMID: 22788238.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GDC-0449, Vismodegib, HhAntag691 supplier, Hedgehog, inhibitors

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