化合物E64FC26 T11141

Product Introduction
Bioactivity


英文名: E64FC26

描述: E64FC26 是一种有效的蛋白质二硫键异构酶 (PDI) 家族泛抑制剂，具有抗肿瘤活性，抑制 PDIA1、PDIA3、PDIA4、TXNDC5 和 PDIA6，可用于研究多发性骨髓瘤和胰腺癌。

体外活性: E64FC26 exhibits anti-multiple myeloma (MM) activity with an EC50 of 0.59 μM after 24 hours of treatment in a concentration range of 0.01-100 μM[1]. E64FC26 demonstrates significant cytotoxicity in a panel of genetically diverse multiple myeloma cell lines (KMS11, OPM2, MM.1S BzR, MM.1S, SA-13, U266 BzR, ANBL6, KMS12PE, U266, 8226 DxR, 8226 BzR, KMS12BM, H929, 8226 cells)[1].

体内活性: In the NSG mouse model, E64FC26 (2 mg/kg; intraperitoneal injection; three times a week for 7 days) demonstrates anti-multiple myeloma (MM) effects, extending the median survival by 2 weeks[1]. The maximum improvement in median survival is observed with both E64FC26 and Bortezomib, leading to a 20-day extension in median survival[1].The pharmacokinetics of E64FC26 were measured in CD-1 mice. E64FC26 was administered via intravenous injection (2 mg/kg; gray trace) or oral administration (5 mg/kg; blue trace), and plasma drug concentrations were measured within 24 hours. In CD-1 mice, after a single oral dose of 5 mg/kg, the maximum concentration (Cmax) reached 400 nM with a terminal half-life of 9.5 hours, demonstrating sufficient oral bioavailability of 34%[1].Vk*MYC transgenic mice were treated with E64FC26 (2 mg/kg, intraperitoneal injection, 3 days/week) for two consecutive weeks. E64FC26 treatment induces an immediate anti-MM response, resulting in an average reduction of 33 ± 7.9% in serum M protein for all mice[1].

存储条件: store at low temperaturePowder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 80 mg/mL (235.03 mM)


关键字: E-64FC26 | E64FC26

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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