| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
CCK2; VEGFR
Nastorazepide targets the gastrin/cholecystokinin-2 (CCK-2) receptor. It is a selective CCK-2 receptor antagonist. By binding to the gastrin/CCK-2 receptor, Nastorazepide prevents receptor activation by gastrin, a peptide hormone. This blocks gastrin-mediated signaling that can lead to the growth of gastric and pancreatic cancer cells. The compound shows high affinity with a Ki of 0.47 nM. |
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| ln Vitro |
In vitro, Nastorazepide inhibits the specific binding of [³H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. It inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, and reduces Akt and NR2B phosphorylation. The compound is a selective CCK-2 receptor antagonist. Detailed in vitro data are available in the primary literature. Nastorazepide is a valuable tool for studying CCK-2 receptor function in cancer.
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| ln Vivo |
In vivo, Nastorazepide is an orally available CCK-2 receptor antagonist with potential antineoplastic activity. It has been evaluated in preclinical models for the treatment of gastric and pancreatic cancer. The compound prevents gastrin-mediated tumor growth. Further in vivo studies are needed to fully characterize its efficacy and safety profile. Nastorazepide is a research compound for oncology applications.
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| Enzyme Assay |
In vitro receptor binding assays for Nastorazepide typically use membrane preparations from cells expressing human CCK-2 receptors. Radioligand binding is performed using [³H]CCK-8 as tracer. Membranes are incubated with radioligand and varying concentrations of Nastorazepide in assay buffer at room temperature for 60-120 minutes. Nonspecific binding is determined using excess unlabeled CCK-8. Bound radioactivity is measured by filtration and scintillation counting. Ki values are calculated from competition curves. Functional assays measure CCK-2 receptor-mediated calcium mobilization or signaling.
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| Cell Assay |
For cell-based assays, cells expressing CCK-2 receptors (e.g., gastric or pancreatic cancer cell lines) are cultured in appropriate medium. Cells are seeded in multi-well plates and treated with Nastorazepide at various concentrations (0.001-10 μM) for 24-72 hours. Cell proliferation is assessed by MTT or CellTiter-Glo. CCK-2 receptor-mediated signaling (e.g., Akt phosphorylation) is assessed by Western blotting. All treatments include vehicle controls and are performed in triplicate.
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| Animal Protocol |
In vivo, Nastorazepide is typically administered orally to rodents. For cancer models, animals bearing gastric or pancreatic tumors are dosed at various regimens. Endpoints include tumor volume measurement, survival analysis, and biomarker assessment. Blood samples are collected for pharmacokinetic analysis. All procedures follow institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Nastorazepide (Z-360, MW 520.62, C₂₉H₃₆N₄O₅) is a selective, orally available CCK-2 receptor antagonist. It has a Ki of 0.47 nM for the human CCK-2 receptor. Detailed pharmacokinetic parameters are available from preclinical studies. The compound is typically stored at -20°C. It is for research purposes.
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| Toxicity/Toxicokinetics |
Nastorazepide is for research use only and not intended for human therapeutic applications. Standard safety pharmacology and toxicology studies would be required for therapeutic development. The compound should be handled with standard laboratory safety precautions. Toxicity data are limited in publicly available sources.
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| References | |
| Additional Infomation |
Nastorazepide (Z-360) is a research-grade selective CCK-2 receptor antagonist for studying cancer and gastrointestinal disorders. Its primary applications include oncology, gastroenterology, and drug discovery. The compound is not approved for clinical use. It is commercially available from various chemical suppliers for research purposes only. Its mechanism involves CCK-2 receptor antagonism and inhibition of gastrin-mediated tumor growth.
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| Molecular Formula |
C29H36N4O5
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|---|---|
| Molecular Weight |
520.61994
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| Exact Mass |
520.268
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| Elemental Analysis |
C, 66.90; H, 6.97; N, 10.76; O, 15.37
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| CAS # |
209219-38-5
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| Related CAS # |
209219-38-5
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| PubChem CID |
9872609
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| Appearance |
White solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
742.8±60.0 °C at 760 mmHg
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| Flash Point |
403.0±32.9 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.631
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| LogP |
5.23
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
38
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| Complexity |
881
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C1[C@@]([H])(C([H])([H])N(C2=C([H])C([H])=C([H])C([H])=C2N1C([H])([H])C(C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=O)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])N([H])C(N([H])C1=C([H])C([H])=C([H])C(C(=O)O[H])=C1[H])=O
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| InChi Key |
VIJCCFFEBCOOIE-JOCHJYFZSA-N
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| InChi Code |
InChI=1S/C29H36N4O5/c1-29(2,3)25(34)18-33-24-15-8-7-14-23(24)32(21-12-5-4-6-13-21)17-22(26(33)35)31-28(38)30-20-11-9-10-19(16-20)27(36)37/h7-11,14-16,21-22H,4-6,12-13,17-18H2,1-3H3,(H,36,37)(H2,30,31,38)/t22-/m1/s1
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| Chemical Name |
3-[[(3R)-1-cyclohexyl-5-(3,3-dimethyl-2-oxobutyl)-4-oxo-2,3-dihydro-1,5-benzodiazepin-3-yl]carbamoylamino]benzoic acid
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| Synonyms |
Z360; Z-360; Z 360; Nastorazepide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~192.07 mM)
Ethanol: ~100 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.00 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9208 mL | 9.6039 mL | 19.2079 mL | |
| 5 mM | 0.3842 mL | 1.9208 mL | 3.8416 mL | |
| 10 mM | 0.1921 mL | 0.9604 mL | 1.9208 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02117258 | Completed | Drug: Z-360 Drug: Placebo |
Metastatic Pancreatic Adenocarcinoma |
Zeria Pharmaceutical | April 2014 | Phase 2 |
| NCT01776463 | Completed | Drug: Z-360 Drug: Placebo |
Healthy Volunteers | Zeria Pharmaceutical | January 2013 | Phase 1 |
| NCT00288925 | Completed | Drug: Z-360 | Pancreatic Cancer | Zeria Pharmaceutical | September 2005 | Phase 1 Phase 2 |
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