Bioactivity | 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-2in 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. | ||||||||||||
Name | Nastorazepide | ||||||||||||
CAS | 209219-38-5 | ||||||||||||
Formula | C29H36N4O5 | ||||||||||||
Molar Mass | 520.62 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Kato H, et al. CCK-2/gastrin receptor signaling pathway is significant for gemcitabine-induced gene expression of VEGF in pancreatic carcinoma cells. Life Sci. 2011 Oct 24;89(17-18):603-8. |