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.
|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|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
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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GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM.
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