Sorafenib is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
|Cell lines||PLC/PRF/5, Hep3B, HepG2, HuH7|
|Preparation method||PLC/PRF/5, Hep3B, HepG2 and HuH7 Cells were seeded in 96-well plates (3,000 cells/well) and incubated overnight for attachment, and were then treated with indicated agents in 10% FBS supplemented medium for 72 hours. The medium was replaced with MTT (0.5 mg/ml) at 37°C for 2 hours. After removal of medium, the cells were lysed with 200 μl per well dimethyl sulfoxide (DMSO), and absorbance at 570 nm was measured and the values of 50% inhibition concentration (IC50) for each drug were determined.|
|Concentrations||0, 0.25, 0.5,1, 2 µM|
|Incubation time||72 hours|
|Animal models||PLC/PRF/5 xenograft model in female athymic nude mice of 4–5 weeks of age|
|Formulation||Dissolved in Cremophor EL/ethanol (50:50; Sigma Cremophor EL, 95% ethanol) at 4 × concentration.|
|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.
|Solubility||DMSO 80 mg/mL|
|Source||Phytomedicine (2015). Figure 1. Sorafenib was purchased from AbMole (Shanghai, China)|
|Method||Cell viability was determined by MTT assay|
|Cell Lines||HCC HepG2|
|Incubation Time||24, 48, 72 hours|
|Results||PPI dose- and time-dependently inhibited the proliferation of HepG2 cells, with IC50 values of 1.047 ± 0.376µM within 24 h. Sorafenib was used as a positive control in HepG2 cells.|
Phytomedicine 2015 Dec 1;1139-49.
Polyphyllin I induced-apoptosis is enhanced by inhibition of autophagy in human hepatocellular carcinoma cells.
Sorafenib purchased from AbMole
Sorafenib and DE605, a novel c-Met inhibitor, synergistically suppress hepatocellular carcinoma
Xiufeng Jiang, et,al. Oncotarget, 2015,6;14.
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