Exherin

Additional information:
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. Note: The old CAT# for this product was 201350A|Product information|CAS Number: 229971-81-7|Molecular Weight: 570.69|Formula: C22H34N8O6S2|Synonym:|ADH-1|ADH1|ADH 1|Chemical Name: (4R,7S,10S,13S,16R)-16-acetamido-13-[(1H-imidazol-5-yl)methyl]-10-methyl-6,9,12,15-tetraoxo-7-(propan-2-yl)-1,2-dithia-5,8,11,14-tetraazacycloheptadecane-4-carboxamide|Smiles: CC(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC2=CN=CN2)NC1=O)C(C)C)C(N)=O|InChiKey: FQVLRGLGWNWPSS-BXBUPLCLSA-N|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|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 2.2 mg/mL (3.85 mM; Need ultrasonic)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Carboplatin} MedChemExpress|{Carboplatin} Autophagy|{Carboplatin} Biological Activity|{Carboplatin} Description|{Carboplatin} manufacturer|{Carboplatin} Epigenetic Reader Domain} |Shelf Life: ≥12 months if stored properly.{{Paliperidone palmitate} medchemexpress|{Paliperidone palmitate} GPCR/G Protein|{Paliperidone palmitate} Technical Information|{Paliperidone palmitate} Data Sheet|{Paliperidone palmitate} manufacturer|{Paliperidone palmitate} Cancer} |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.PMID:24360118 |Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|ADH-1 (0.2 mg/mL) blocks collagen I-mediated changes in pancreatic cancer cells, and is highly effective at preventing cell motility that is induced by expression of N-cadherin. ADH-1 (0, 0.1, 0.2, 0.5 and 1.0 mg/mL) induces apoptosis in a dose-dependent and N-cadherin-dependent manner.|In Vivo:|ADH-1 (50 mg/kg) significantly prevents tumor growth and metastasis in a mouse model for pancreatic cancer. ADH-1 prevents tumor cell invasion and metastasis in an orthotopic model for pancreatic cancer using N-cadherin overexpressing BxPC-3 cells. ADH-1, at the dosages evaluated, does not display either antiangiogenic activity in a rat aortic ring assay or antitumor potential in a PC3 subcutaneous xenograft tumor model. ADH-1 (10 mL/kg, i.p.) augmentation of melanoma tumor growth is overcome through its ability to make regionally infused melphalan more effective. ADH-1 mediated augmentation of melanoma tumor growth is not altered by regionally infused temozolomide. In A375, but not DM443 xenografts, ADH-1 treatment increases phosphorylation of AKT at serine 473. ADH-1 slightly diminishes N-cadherin expression in both xenografts.|References:|Li H, et al. ADH1, an N-cadherin inhibitor, evaluated in preclinical models of angiogenesis and androgen-independent prostate cancer. Anticancer Drugs. 2007 Jun;18(5):563-8.Turley RS, et al. Targeting N-cadherin increases vascular permeability and differentially activates AKT in melanoma. Ann Surg. 2015 Feb;261(2):368-77Products are for research use only. Not for human use.|