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E64FC26

CAS No. : 2285446-62-8

MCE 站：E64FC26

产品活性：E64FC26 是蛋白质二硫键异构酶 (PDI) 家族的一种有效的泛抑制剂，对 PDIA1、PDIA3、PDIA4、TXNDC5 和 PDIA6 的 IC₅₀ 分别为 1.9、20.9、25.9、16.3 和 25.4 μM。E64FC26 显示抗骨髓瘤活性。

研究领域：Apoptosis

作用靶点：Apoptosis

In Vitro: E64FC26 (0.01-100 ?M; 24 hours) shows anti-MM activity , with an EC₅₀ of 0.59 μM.E64FC26 is more cytotoxic against a genetically diverse panel of multiple myeloma (MM) cell lines (KMS11, OPM2, MM.1S BzR, MM.1S, SA-13, U266 BzR, ANBL6, KMS12PE, U266, 8226 DxR, 8226 BzR, KMS12BM, H929,8226 cells) when compared to non-malignant cells.

In Vivo: E64FC26 (2 mg/ kg; i.p.; three days a week for 7days) shows anti-MM effect in NSG mice model, and increases median survival by 2 weeks.
The combination of E64FC26 and Bortezomib produced the greatest improvement in survival, extending the median survival by 20 days.
Pharmacokinetic of E64FC26 was measured in CD-1 mice. E64FC26 was administered i.v. (2 mg/kg; gray tracing) or p.o. (5 mg/ kg; blue tracing) and plasma drug concentrations were measured over a 24 h period. In CD-1 mice demonstrated adequate oral bioavailabilty of 34% with systemic exposure approaching a maximum concentration (Cmax) of 400 nM after a single oral dose of 5 mg/kg with a terminal half-life of 9.5 h.
Vk*MYC transgenic mice are treated with E64FC26 (2 mg/kg, i.p., 3 days/week) for two consecutive weeks. E64FC26 treatment induces an immediate anti-MM response, decreasing serum M-protein in all mice by an average of 33 ± 7.9%.

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