SGI-7079 is a novel Axl inhibitor. SGI-7079 decreased IBC cell proliferation, migration and invasion in vitro and inhibited tumor growth of IBC cells in vivo. Mesenchymal cells also expressed increased levels of the receptor tyrosine kinase Axl and showed a trend toward greater sensitivity to the Axl inhibitor SGI-7079, whereas the combination of SGI-7079 with erlotinib reversed erlotinib resistance in mesenchymal lines expressing Axl and in a xenograft model of mesenchymal NSCLC.
 |
Source | Cancer Res (2013). Figure 6. SGI-7079 |
| Method | MTT | |
| Cell Lines | SUM149 cells | |
| Concentrations | 1 mmol/L | |
| Incubation Time | 72 h | |
| Results | SGI-7079 treatment inhibited the phosphorylation of Axl at Tyr 702 upon Gas6 stimulation in SUM149 cells |
| Cell Experiment | |
|---|---|
| Cell lines | Mouse ID8 ovarian cancer, TC1 lung cancer, 4T1 breast cancer and CT26 colorectal cancer cells |
| Preparation method | Cell proliferation assay Cells were plated in 96-well plates (5 × 103/well) and then transfected with siNC or siAxl using Lipofectamine 2000 according to the manufacturer's instructions or treated with vehicle, R428 or SGI-7079 at indicated concentrations. After 72 hours of treatment, cell proliferation assays were performed using Cell Counting Kit-8 according to the manufacturer's instructions. Absorbance was measured at 490 nm using a microplate reader (Molecular devices). The percentage of cell survival was defined as the relative absorbance of untreated versus treated cells. |
| Concentrations | - |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | BALB/c syngeneic mice or nude mice |
| Formulation | formulated in 0.5% hydroxypropylmethylcellulose plus 0.1% Tween 80 |
| Dosages | 50 mg/kg |
| Administration | orally |
| Molecular Weight | 455.53 |
| Formula | C26H26FN7 |
| CAS Number | 1239875-86-5 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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