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Nenocorilantis a potent, orally activity glucocorticoid receptor (GR) antagonist with Ki value of 0.15 nM. Nenocorilant has pro-apoptotic effects and improves potency combined with cytotoxic agent.
Nenocorilant (0-1000 nM; 0-72 h; OvCa cells) has pro-apoptotic effects and reverses the effects of cortisol and partially restored Paclitaxel and Gemcitabine induction of tumor-cell apoptosis. Nenocorilant (100 nM; 4 h; MIA PaCa-2 and OVCAR5 cells) prevents dex-mediated upregulation of both GR target genes SGK1 and MKP1.
Nenocorilant (30 mg/kg; p.o.; once every four days, for 25 d; female Balb/c nude mice) improves the efficacy and promotes apoptotic activity of cytotoxic therapy in xenograft models under physiological cortisol conditions.
| Molecular Weight | 587.55 |
| Formula | C26H21F4N7O3S |
| CAS Number | 1496509-78-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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