英文同义词:
ADH 1;Exherin;Exherin TFA;Exherin (ADH-1);ADH-1 Exherin;CS-2142;L-Cysteinamide, N-acetyl-L-cysteinyl-L-histidyl-L-alanyl-L-valyl-, cyclic (1→5)-disulfide
相关类别:
小分子抑制剂;小分子抑制剂,天然产物;抑制剂;Inhibitors;API
储存条件
Keep in dark place,Sealed in dry,Store in freezer, under -20°C
生物活性
ADH-1 是一种 N-cadherin 的拮抗剂,能够抑制 N-cadherin 介导的细胞黏附。
体外研究
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.
体内研究
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.