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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.
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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 |
| Related TAM Receptor Products |
|---|
| Bemcentinib
Bemcentinib (R428) is a potent and selective small-molecule inhibitor of Axl kinase with IC50 of 14 nM. |
| UNC2250
UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3. |
| UNC2881
UNC2881 is a specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively |
| Dubermatinib
Dubermatinib (TP-0903) is a potent and selective AXL inhibitor with an IC50 value of 27 nM. |
| RU-301
RU-301 is a pan-TAM receptor inhibitor that blocks Gas6-induced TAM activation and tumorigenicity, with Kd and IC50 values of 12 μM and 10 μM, respectively. |
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