E64FC26

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E64FC26

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2285446-62-8

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
200mg	电议
500mg	电议

产品介绍

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。

生物活性

E64FC26 is a potent pan-inhibitor of theprotein disulfide isomerase (PDI)family, withIC₅₀s of 1.9, 20.9, 25.9, 16.3, and 25.4 μM against PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6, respectively. E64FC26 shows anti-myeloma activity^[1].

体外研究
(In Vitro)

E64FC26 (0.01-100 μM; 24 hours) shows anti-MM activity , with an EC₅₀of 0.59 μM^[1]. 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^[1].

Cell Viability Assay^[1]

Cell Line:	MM.1S BzR cells
Concentration:	0.01, 0.1, 1, 10, 100 μM
Incubation Time:	24 hours
Result:	Showed anti-MM activity , with an EC₅₀of 0.59 μM.

体内研究
(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^[1].
The combination of E64FC26 and Bortezomib produced the greatest improvement in survival, extending the median survival by 20 days^[1].
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^[1].
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%^[1].

Animal Model:	NOD-SCID IL2Rγ-/- (NSG) mice (bearing MM.1S cells)^[1]
Dosage:	2 mg/ kg
Administration:	i.p.; three days a week for 7days
Result:	Showed a clear anti-MM effect in this model also, increasing median survival by 2 weeks.

分子量

340.38

性状

Solid

Formula

C₁₉H₂₃F₃O₂

CAS 号

2285446-62-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL(293.79 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.9379 mL	14.6895 mL	29.3789 mL
5 mM	0.5876 mL	2.9379 mL	5.8758 mL
10 mM	0.2938 mL	1.4689 mL	2.9379 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline)
Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.34 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在本网站选购。