| 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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| 250mg |
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Nastorazepide, formerly known as Z-360, is a selective, orally bioavailable, 1,5-benzodiazepine-analogue gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. Z-360 attaches itself to the gastrin/CCK-2 receptor, blocking the peptide hormone gastrin from activating the receptor and often leading to the growth of gastric and pancreatic cancer cells.
| Molecular Formula |
C29H36N4O5
|
|---|---|
| Molecular Weight |
520.61994
|
| Exact Mass |
520.268
|
| Elemental Analysis |
C, 66.90; H, 6.97; N, 10.76; O, 15.37
|
| CAS # |
209219-38-5
|
| Related CAS # |
209219-38-5
|
| PubChem CID |
9872609
|
| Appearance |
White solid powder
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| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
742.8±60.0 °C at 760 mmHg
|
| Flash Point |
403.0±32.9 °C
|
| Vapour Pressure |
0.0±2.6 mmHg at 25°C
|
| Index of Refraction |
1.631
|
| LogP |
5.23
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
38
|
| Complexity |
881
|
| Defined Atom Stereocenter Count |
1
|
| 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
|
| InChi Key |
VIJCCFFEBCOOIE-JOCHJYFZSA-N
|
| 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
|
| 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
|
| 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)
|
| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~192.07 mM)
Ethanol: ~100 mg/mL |
|---|---|
| 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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