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SC144 is the first oral active GP130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, eliminates Stat3 phosphorylation and nuclear translocation, and further inhibits downstream target gene expression. SC144 inhibited signal transduction induced by GP130 ligand. SC144 induces apoptosis of human ovarian cancer cells.
| Cell Experiment | |
|---|---|
| Cell lines | OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY NCI/ADR-RES |
| Preparation method | MTT assay |
| Concentrations | ~10 μM |
| Incubation time | 96 h |
| Animal Experiment | |
|---|---|
| Animal models | Human Ovarian Cancer OVCAR-8 Xenograft |
| Formulation | .9% NaCl with 40% propylene glycol |
| Dosages | 10 mg/kg daily |
| Administration | i.p. or p.o. |
| Molecular Weight | 322.3 |
| Formula | C16H11FN6O |
| CAS Number | 895158-95-9 |
| Form | Solid |
| Solubility (25°C) | DMSO 15 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[4] Takashi Oshima, et al. Combination effects of SC144 and cytotoxic anticancer agents
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