化合物Exherin trifluoroacetate T1608

Product Introduction
Bioactivity


英文名: ADH-1 trifluoroacetate

描述: ADH-1 trifluoroacetate (Exherin trifluoroacetate) 是一种选择性的、竞争性N-钙粘蛋白拮抗剂，具有潜在抗肿瘤和抗血管生成作用。

动物实验: 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.

体外活性: 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.

体内活性: 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].

存储条件: keep away from moisturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 43 mg/mL


关键字: ADH 1 | ADH1 trifluoroacetate | Inhibitor | Exherin Trifluoroacetate | ADH1 | ADH-1 Trifluoroacetate | ADH-1 | ADH 1 Trifluoroacetate | inhibit | ADH 1 trifluoroacetate | ADH1 Trifluoroacetate

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相关库: Drug Repurposing Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Fluorochemical Library | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | NO PAINS Compound Library | Covalent Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途