Exherin - CAS 229971-81-7
Catalog number:
229971-81-7
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
Others
Description:
Exherin, also known as ADH-1, is a small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor vasculature, inhibition of tumor cell growth, and the induction of tumor cell and endothelial cell apoptosis. N-cadherin, a cell- surface transmembrane glycoprotein of the cadherin superfamily of proteins involved in calcium-mediated cell-cell adhesion and signaling mechanisms; may be upregulated in some aggressive tumors and the endothelial cells and pericytes of some tumor blood vessels.
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Appearance:
white solid powder
Synonyms:
NSC729477; ADH-1. Brand name: Exherin.
MSDS:
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Current Developer:
Adherix Technologies, Inc.
1.Phase I clinical trial of Exherin (ADH-1) in patients with advanced solid tumors.
Yarom N1, Stewart D, Malik R, Wells J, Avruch L, Jonker DJ. Curr Clin Pharmacol. 2013 Feb 1;8(1):81-8.
ADH-1 (Exherin™) is a pentapeptide, which competitively inhibits N-cadherin, resulting in vascular disruptive effect of tumor vasculature in preclinical models. This study was designed to assess the toxicity of ADH-1 and to determine the maximal tolerated dose (MTD).
2.Clinical and pharmacological phase I evaluation of Exherin (ADH-1), a selective anti-N-cadherin peptide in patients with N-cadherin-expressing solid tumours.
Perotti A1, Sessa C, Mancuso A, Noberasco C, Cresta S, Locatelli A, Carcangiu ML, Passera K, Braghetti A, Scaramuzza D, Zanaboni F, Fasolo A, Capri G, Miani M, Peters WP, Gianni L. Ann Oncol. 2009 Apr;20(4):741-5. doi: 10.1093/annonc/mdn695. Epub 2009 Feb 3.
BACKGROUND: Upregulation of N-cadherin promotes dysregulated cell growth, motility, invasiveness, plus maintenance of vascular stability and is associated with cancer progression in several human tumour types. N-cadherin is expressed also on tumour cells and the anti-N-cadherin cyclic pentapeptide ADH-1, tested in the present study, can exert a direct antitumour effect.
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CAS 229971-81-7 Exherin

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