Cas No.: | 209219-38-5 |
Chemical Name: | Benzoic acid, 3-[[[[(3R)-5-cyclohexyl-1-(3,3-dimethyl-2-oxobutyl)-2,3,4,5-tetrahydro-2-oxo-1H-1,5-benzodiazepin-3-yl]amino]carbonyl]amino]- |
Synonyms: | Nastorazepide |
SMILES: | O=C(C1C=C(NC(=O)NC2CN(C3CCCCC3)C3C(=CC=CC=3)N(CC(=O)C(C)(C)C)C2=O)C=CC=1)O |
Formula: | C29H36N4O5 |
M.Wt: | 520.6199 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | A novel potent, orally active CCK-2/gastrin receptor antagonist with Ki of 0.47 nM; significantly reduces gastrin-induced PKB/Akt phosphorylation in human CCK-2 receptor-expressing cells; significantly inhibits the growth of MiaPaCa2, also suppresses pancreatic tumor growth and prolong survival in a pancreatic carcinoma xenograft model combined with gemcitabine; prevents up-regulation of ephrin B1 gene expression and phosphorylation of NR2B via suppression of interleukin-1 β production in a cancer-induced pain model in mice.Pancreatic CancerPhase 2 Clinical |