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Nastorazepide (Z-360) is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. Target：CCK-2 in vitro: Z-360 binds to the gastrin/CCK-2 receptor, thereby preventing receptor activation by gastrin, a peptide hormone frequently associated with the proliferation of gastrointestinal and pancreatic tumor cells. Check for active clinical trials or closed clinical trials using this agent. in vivo: Z-360 is a novel orally active CCK-2/gastrin receptor antagonist, significantly inhibits the growth of subcutaneous xenografts of human pancreatic tumor cells in mice, and that Z-360 combined with gemcitabine prolonged survival in a pancreatic carcinoma orthotopic xenograft mice.
| Molecular Weight | 520.62 |
| Formula | C29H36N4O5 |
| CAS Number | 209219-38-5 |
| Form | Solid |
| Solubility (25°C) | DMSO ≥ 32 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Doroteja Novak, et al. Drug Discov Today. CCK2R antagonists: from SAR to clinical trials
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Tetragastrin (Cholecystokinin tetrapeptide; CCK-4) is the C-terminal tetrapeptide of gastrin. |
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