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

Product Specifications

CAS Number

[209219-38-5]

Product Name Alternative

Z-360

UNSPSC

12352005

Hazard Statement

H315, H317, H318, H334, H335, H341, H361, H370, H413

Target

Akt; Cholecystokinin Receptor; Ephrin Receptor; HIF/HIF Prolyl-Hydroxylase; Interleukin Related; VEGFR

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Metabolic Enzyme/Protease; Neuronal Signaling; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Nastorazepide.html

Purity

99.95

Solubility

DMSO : ≥ 32 mg/mL

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

Molecular Formula

C29H36N4O5

Molecular Weight

520.62

Precautions

H315, H317, H318, H334, H335, H341, H361, H370, H413

References & Citations

[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.|[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.|[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. |[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. |[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.|[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. |[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.