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ADH-1 trifluoroacetate

Catalog No. T1608   CAS 1135237-88-5
Synonyms: Exherin trifluoroacetate

ADH-1 trifluoroacetate (Exherin trifluoroacetate) is a 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.

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ADH-1 trifluoroacetate Chemical Structure
ADH-1 trifluoroacetate, CAS 1135237-88-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 44.00
5 mg In stock $ 98.00
10 mg In stock $ 160.00
25 mg In stock $ 298.00
50 mg In stock $ 423.00
100 mg In stock $ 627.00
1 mL * 10 mM (in DMSO) In stock $ 160.00
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Purity: 99.17%
Purity: 98%
Purity: 98%
Purity: 98%
Purity: 96.64%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description ADH-1 trifluoroacetate (Exherin trifluoroacetate) is a 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.
In vitro In pancreatic cancer cells, Exherin (0.2 mg/mL) blocks collagen I-mediated changes and is highly potent at preventing cell motility induced by expression of N-cadherin. Exherin (0-1.0 mg/mL) dose-dependently induces apoptosis in a N-cadherin-dependent manner.
In vivo In a mouse model for pancreatic cancer, Exherin (50 mg/kg) markedly inhibits tumor growth and metastasis [1]. In a rat aortic ring assay or antitumor potential in a PC3 subcutaneous xenograft tumor model, Exherin does not display either antiangiogenic activity [2]. The augmentation of melanoma tumor growth mediated by Exherin is not altered by regionally infused temozolomide. In A375, but not DM443 xenografts, Exherin can increase phosphorylation of AKT at serine 473. Exherin slightly diminishes N-cadherin expression in both xenografts[3].
Animal Research Exherin is prepared in PBS.Animals are anesthetized, and 40 μL of a single cell suspension containing 50,000 cells is injected into the pancreas. Mice are randomized into treatment groups 10 days after surgery. For treatment, mice are injected intraperitoneally once per day with Exherin at 50 mg/kg in 100 μL PBS (×1 per day, ×5 per week for 4 weeks). For in vivo bioluminescence, D-Luciferin is administered by intraperitoneal injection. Data are acquired 20 min after injection using the IVIS system. Tumor growth is monitored every 10 days from day 10 to day 50 after surgery. Luciferase activity is quantified using the IVIS system. Two months after surgery, the mice are killed, and the pancreas, liver, lung, and disseminated nodules are harvested, fixed in 10% buffered formalin, and embedded in paraffin. Serial 5-μM sections are cut, mounted on slides, and stained with H&E using standard procedures.
Synonyms Exherin trifluoroacetate
Molecular Weight 684.71
Formula C24H35F3N8O8S2
CAS No. 1135237-88-5

Storage

keep away from moisture

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 43 mg/mL

TargetMolReferences and Literature

1. Shintani Y, et al. ADH-1 suppresses N-cadherin-dependent pancreatic cancer progression. Int J Cancer. 2008 Jan 1;122(1):71-7. 2. 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. 3. Turley RS, et al. Targeting N-cadherin increases vascular permeability and differentially activates AKT in melanoma. Ann Surg. 2015 Feb;261(2):368-77.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Covalent Inhibitor Library Bioactive Compound Library Bioactive Compounds Library Max Fluorochemical Library Anti-Metabolism Disease Compound Library

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Keywords

ADH-1 trifluoroacetate 1135237-88-5 Metabolism Dehydrogenase Exherin trifluoroacetate ADH 1 ADH1 trifluoroacetate Inhibitor Exherin Trifluoroacetate ADH1 ADH-1 Trifluoroacetate ADH-1 ADH 1 Trifluoroacetate inhibit ADH 1 trifluoroacetate ADH1 Trifluoroacetate inhibitor

 

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