Need Assistance?

US & Canada:
+
UK: +

Our Highlights

GMP Grade Efficient workshop for GMP production.
Optimal Prices Buying products on this site guarantees the best price!
Commercial Batches Independent GMP manufacturing suites that handle commercial batches
Prompt Delivery Warehouses in multiple cities to ensure timely delivery
Flexible Quantity Quantities available from milligrams to ton

Exherin

* Please kindly note that our products are not to be used for therapeutic purposes and cannot be sold to patients.

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.

Category

Peptide Inhibitors

Catalog number

BAT-010745

CAS number

229971-81-7

Molecular Formula

C22H34N8O6S2

Molecular Weight

570.69

Size	Price	Stock	Quantity
10 mg	$197	In stock

Specification
Reference Reading

IUPAC Name

(4R,7S,10S,13S,16R)-16-acetamido-13-(1H-imidazol-5-ylmethyl)-10-methyl-6,9,12,15-tetraoxo-7-propan-2-yl-1,2-dithia-5,8,11,14-tetrazacycloheptadecane-4-carboxamide

Synonyms

NSC729477; ADH-1; NSC7 29477; ADH 1; NSC-729477; ADH1

Related CAS

1135237-88-5 (trifluoroacetate)

Appearance

white solid powder

Purity

98%

Density

1.4±0.1 g/cm3

Boiling Point

1183.4±65.0°C at 760 mmHg

Sequence

Ac-Cys(1)-His-Ala-Val-Cys(1)-NH2

Storage

Store at -20°C

Solubility

Soluble in DMSO

InChI

InChI=1S/C22H34N8O6S2/c1-10(2)17-22(36)29-15(18(23)32)7-37-38-8-16(27-12(4)31)21(35)28-14(5-13-6-24-9-25-13)20(34)26-11(3)19(33)30-17/h6,9-11,14-17H,5,7-8H2,1-4H3,(H2,23,32)(H,24,25)(H,26,34)(H,27,31)(H,28,35)(H,29,36)(H,30,33)/t11-,14-,15-,16-,17-/m0/s1

InChI Key

FQVLRGLGWNWPSS-BXBUPLCLSA-N

Canonical SMILES

CC1C(=O)NC(C(=O)NC(CSSCC(C(=O)NC(C(=O)N1)CC2=CN=CN2)NC(=O)C)C(=O)N)C(C)C

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.