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Cat. No. M1713
GDC-0449 Structure

Vismodegib, HhAntag691

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL In DMSO USD 55 In stock
10mg USD 60 In stock
50mg USD 90 In stock
100mg USD 130 In stock
200mg USD 190 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.

Customer Product Validations & Biological Datas
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
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
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 99.49%
Solubility DMSO 64 mg/mL
Storage at -20°C

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

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