est-64454

EST64454 Maleic acid salt 是EST64454的马来酸盐形式。EST64454是一种用于治疗疼痛的高可溶性σ1受体拮抗剂临床候选药物。

EST64454 hydrochloride (EST64454) 是一种可口服的选择性sigma-1受体拮抗剂，Ki 为 22 nM。它有用于疼痛的研究潜力。

EST64454 is a σ1 receptor (σ1R) antagonist clinical candidate for the treatment of pain. EST64454 shows an outstanding aqueous solubility, which together with its high permeability in Caco-2 cells will allow its classification as a BCS class I compound. It also shows high metabolic stability.

EHT-6706 is a novel microtubule-disrupting agent that targets the colchicine-binding site to inhibit tubulin polymerization. At low nM concentrations, EHT 6706 exhibits highly potent antiproliferative activity on more than 60 human tumor cell lines, even those described as being drug resistant. EHT 6706 also shows strong efficacy as a vascular-disrupting agent, since it prevents endothelial cell tube formation and disrupts pre-established vessels, changes the permeability of endothelial cell monolayers and inhibits endothelial cell migration. Genome-wide transcriptomic analysis of EHT 6706 effects on human endothelial cells shows that the antiangiogenic activity elicits gene deregulations of antiangiogenic pathways. These findings indicate that EHT 6706 is a promising tubulin-binding compound with potentially broad clinical antitumor efficacy.