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.

Physicochemical Properties

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
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
HS Tariff Code	2934.99.9001
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)

Biological Activity

Targets	CCK2; VEGFR
References	[1]. 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.

Solubility Data

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.