2. GPCR/G Protein Neuronal Signaling Protein Tyrosine Kinase/RTK Immunology/Inflammation Metabolic Enzyme/Protease PI3K/Akt/mTOR
  3. Cholecystokinin Receptor Ephrin Receptor Interleukin Related VEGFR HIF/HIF Prolyl-Hydroxylase Akt
  4. Nastorazepide

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 Ki 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.

For research use only. We do not sell to patients.

Nastorazepide Chemical Structure

Nastorazepide Chemical Structure

CAS No. : 209219-38-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Other Forms of Nastorazepide:

Nastorazepide Related Antibodies

Top Publications Citing Use of Products

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CCKAR CCKBR

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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 Ki 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[1][2][3][4][5][6][7].

IC50 & Target

CCKBR

 

In Vitro

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 Ki 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[1][2][3][4][5][6][7].

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

Nastorazepide Related Antibodies
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
Molecular Weight

520.62

Formula

C29H36N4O5
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

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

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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • 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:

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mg/kg

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(per animal)

g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.95%

SDS (583 KB)

COA (257 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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Nastorazepide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Nastorazepide209219-38-5Z-360Z360Z 360Cholecystokinin ReceptorEphrin ReceptorInterleukin RelatedVEGFRHIF/HIF Prolyl-HydroxylaseAktCCK ReceptorILVascular endothelial growth factor receptorHypoxia-inducible factorsHIFsHIF-PHPKBProtein kinase BC170HM2MGLVA1 ascitesMIA PaCa-2micenociceptive responsesInhibitorinhibitorinhibit

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