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E64FC26

产品编号 T11141 CAS 2285446-62-8

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。

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E64FC26, CAS 2285446-62-8

规格	价格/CNY		货期	数量
1 mg	￥ 1,650		现货
5 mg	￥ 5,799		现货

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其他形式的 E64FC26:

(E/Z)-E64FC26
询价

选择批次

纯度: 98.1%

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	E64FC26 is a potent protein disulfide isomerase (PDI) family pan-inhibitor with antitumor activity, inhibits PDIA1, PDIA3, PDIA4, TXNDC5 and PDIA6, and can be used in the study of multiple myeloma and pancreatic cancer.
靶点活性	anti-multiple myeloma:0.59 μM (EC50)
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].

分子量	340.38
分子式	C19H23F3O2
CAS No.	2285446-62-8

存储

store at low temperature　|　Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 80 mg/mL (235.03 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9379 mL	14.6895 mL	29.3789 mL	73.4473 mL
	5 mM	0.5876 mL	2.9379 mL	5.8758 mL	14.6895 mL
	10 mM	0.2938 mL	1.4689 mL	2.9379 mL	7.3447 mL
	20 mM	0.1469 mL	0.7345 mL	1.4689 mL	3.6724 mL
	50 mM	0.0588 mL	0.2938 mL	0.5876 mL	1.4689 mL
	100 mM	0.0294 mL	0.1469 mL	0.2938 mL	0.7345 mL

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参考文献

1. Robinson RM, et al. Inhibitors of the protein disulfide isomerase family for the treatment of multiple myeloma. Leukemia. 2019 Apr;33(4):1011-1022.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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