Art. -Nr.: HY-17617

Nastorazepide

(Synonyms: Z-360)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [³H]CCK-8 to the human CCK-2 receptor with a K_i value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain.

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Reinheit: 99.95%
CAS. Nr.: 209219-38-5
Formel: C₂₉H₃₆N₄O₅
Molecular Weight:520.62

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Nastorazepide Chemical Structure

CAS. Nr.: 209219-38-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

CCKBR

Alle Cholecystokinin Receptor Isoform-spezifische Produkte anzeigen :

CCKAR
CCKBR

Alle Ephrin Receptor Isoform-spezifische Produkte anzeigen :

EphB
EphA

Alle Interleukin Related Isoform-spezifische Produkte anzeigen :

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen :

Alle Akt Isoform-spezifische Produkte anzeigen :

In Vitro

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Nastorazepide (10-100 mg/kg; p.o.; once daily; 21 days) significantly inhibits tumor growth in a dose-dependent manner in subcutaneous xenograft model of MiaPaCa2 cells in nude mice^[2].
Nastorazepide (3-100 mg/kg; p.o.; once daily) inhibits colorectal cancer liver metastasis in the C170HM2 mouse model, increases survival in the MGLVA1 ascites mouse model, and inhibits pancreatic tumor growth when combined with Gemcitabine in the PAN-1 orthotopic mouse model^[3].
Nastorazepide (100 mg/kg; p.o.; once daily; 3 weeks) suppresses tumor growth in MIA PaCa-2-bearing mice via inhibition of Gastrin-induced anti-apoptotic effects^[4].
Nastorazepide (30-300 mg/kg; p.o.; starting from day 7 and continuing until day 21 in the cancer pain model) can inhibit the late-phase nociceptive responses in the Formalin-induced pain model, produce an anti-allodynic effect in the cancer pain model^[5].
Nastorazepide (100 mg/kg; p.o.; once daily; from day 7 to day 14) prevents up-regulation of ephrin B1 gene expression and phosphorylation of NR2B via suppression of IL-1β production in a cancer-induced pain model in mice^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c-nu/nuSlc nude mice (female, 7-week-old) with subcutaneous xenograft of MiaPaCa2 cells^[2]
Dosage:

10 mg/kg, 30 mg/kg, 100 mg/kg
Administration:

Oral administration, once daily, for 21 days
Result:

Significantly inhibited tumor growth of MiaPaCa2 subcutaneous xenografts in a dose-dependent manner.
Resulted in final tumor weight inhibition of 16.5%, 39.6%, and 41.7% at 10, 30, and 100 mg/kg, respectively.

Animal Model:

Nude mice with PAN-1 orthotopic pancreatic model^[3]

Dosage:

30 mg/kg, 100 mg/kg

Administration:

Oral gavage (p.o.), once daily

Result:

Did not suppress basal tumor area or weight at all doses when used as monotherapy.
Inhibited both tumor area and weight when used in combination with Gemcitabine.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 209219-38-5
Appearance Solid
Molecular Weight 520.62
Formel C₂₉H₃₆N₄O₅
Color White to off-white
SMILES

O=C(O)C1=CC=CC(NC(N[C@H]2C(N(CC(C(C)(C)C)=O)C3=CC=CC=C3N(C4CCCCC4)C2)=O)=O)=C1
Synonyms

Z-360
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

bioRxiv

2026 May 7.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 32 mg/mL (61.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (4.00 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.00 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (284 KB)
SDS (583 KB)
- English - EN (583 KB)
- Français - FR (583 KB)
- Deutsch - DE (583 KB)
- Norwegian - NO (583 KB)
- Español - ES (583 KB)
- Swedish - SV (583 KB)
- Italian - IT (583 KB)
- Portuguese - PT (583 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[2]. Kawasaki D, et al. Effect of Z-360, a novel orally active CCK-2/gastrin receptor antagonist on tumor growth in human pancreatic adenocarcinoma cell lines in vivo and mode of action determinations in vitro. Cancer Chemother Pharmacol. 2008 Apr;61(5):883-92. [Content Brief]

[3]. Grabowska AM, et al. Pre-clinical evaluation of a new orally-active CCK-2R antagonist, Z-360, in gastrointestinal cancer models. Regul Pept. 2008 Feb 7;146(1-3):46-57. [Content Brief]

[4]. Shiomi Y, et al. Z-360 Suppresses Tumor Growth in MIA PaCa-2-bearing Mice via Inhibition of Gastrin-induced Anti-Apoptotic Effects. Anticancer Res. 2017 Aug;37(8):4127-4137. [Content Brief]

[5]. Yoshinaga K, et al. Pharmacological evaluation of analgesic effects of the cholecystokinin2 receptor antagonist Z-360 in mouse models of formalin- and cancer-induced pain. Biol Pharm Bull. 2010;33(2):244-8. [Content Brief]

[6]. Orikawa Y, et al. Z-360, a novel therapeutic agent for pancreatic cancer, 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. Mol Pain. 2010 Oct 28;6:72. [Content Brief]

[7]. Kobayashi N, et al. Z-360, a novel cholecystokinin-2/gastrin receptor antagonist, inhibits gemcitabine-induced expression of the vascular endothelial growth factor gene in human pancreatic cancer cells. Biol Pharm Bull. 2010;33(2):216-22. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9208 mL	9.6039 mL	19.2079 mL	48.0197 mL
	5 mM	0.3842 mL	1.9208 mL	3.8416 mL	9.6039 mL
	10 mM	0.1921 mL	0.9604 mL	1.9208 mL	4.8020 mL
	15 mM	0.1281 mL	0.6403 mL	1.2805 mL	3.2013 mL
	20 mM	0.0960 mL	0.4802 mL	0.9604 mL	2.4010 mL
	25 mM	0.0768 mL	0.3842 mL	0.7683 mL	1.9208 mL
	30 mM	0.0640 mL	0.3201 mL	0.6403 mL	1.6007 mL
	40 mM	0.0480 mL	0.2401 mL	0.4802 mL	1.2005 mL
	50 mM	0.0384 mL	0.1921 mL	0.3842 mL	0.9604 mL
	60 mM	0.0320 mL	0.1601 mL	0.3201 mL	0.8003 mL

Keywords

Nastorazepide

1 Cited Publications

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Nastorazepide

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Publications Citing Use of MedChemExpress (MCE) Nastorazepide

Alle Cholecystokinin Receptor Isoform-spezifische Produkte anzeigen

Alle Ephrin Receptor Isoform-spezifische Produkte anzeigen

Alle Interleukin Related Isoform-spezifische Produkte anzeigen

Alle VEGFR Isoform-spezifische Produkte anzeigen

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen

Alle Akt Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation