Nastorazepide

• 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].

• 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  CCKBR

• CAS Number :

  [209219-38-5]