Art. -Nr.: HY-122895

E64FC26

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

E64FC26 is a potent pan-inhibitor of the protein disulfide isomerase (PDI) family, with IC₅₀s 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.

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Reinheit: 98.48%
CAS. Nr.: 2285446-62-8
Formel: C₁₉H₂₃F₃O₂
Molecular Weight:340.39

Speicherung:

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

E64FC26 Chemical Structure

CAS. Nr.: 2285446-62-8

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

E64FC26 (0.01-100 μM; 24 hours) shows anti-MM activity , with an EC₅₀ of 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 EC₅₀ of 0.59 μM.

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 (C_max) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS. Nr. 2285446-62-8
Appearance Solid
Molecular Weight 340.39
Formel C₁₉H₂₃F₃O₂
Color Light yellow to yellow
SMILES

OC1=CC2=C(/C(C=C2C(F)(F)F)=C/CCCCCCCC)C=C1O.[(E)]
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (2)

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Journal Impact Factor

Int J Mol Sci

Pan-Inhibition of Protein Disulfide Isomerase Caused Cell Death through Disrupting Cellular Proteostasis in Pancreatic Ductal Adenocarcinoma Cells. [Abstract]

2023 Nov 17;24(22):16467. PMID: 38003657
J Virol

Hepatitis E virus ORF3 protein hijacking thioredoxin domain-containing protein 5 (TXNDC5) for its stability to promote viral particle release. [Abstract]

2024 Apr 16;98(4):e0164923. PMID: 38548704

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (293.78 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9378 mL

14.6890 mL

29.3781 mL

5 mM

0.5876 mL

2.9378 mL

5.8756 mL

10 mM

0.2938 mL

1.4689 mL

2.9378 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9378 mL	14.6890 mL	29.3781 mL	73.4452 mL
	5 mM	0.5876 mL	2.9378 mL	5.8756 mL	14.6890 mL
	10 mM	0.2938 mL	1.4689 mL	2.9378 mL	7.3445 mL
	15 mM	0.1959 mL	0.9793 mL	1.9585 mL	4.8963 mL
	20 mM	0.1469 mL	0.7345 mL	1.4689 mL	3.6723 mL
	25 mM	0.1175 mL	0.5876 mL	1.1751 mL	2.9378 mL
	30 mM	0.0979 mL	0.4896 mL	0.9793 mL	2.4482 mL
	40 mM	0.0734 mL	0.3672 mL	0.7345 mL	1.8361 mL
	50 mM	0.0588 mL	0.2938 mL	0.5876 mL	1.4689 mL
	60 mM	0.0490 mL	0.2448 mL	0.4896 mL	1.2241 mL
	80 mM	0.0367 mL	0.1836 mL	0.3672 mL	0.9181 mL
	100 mM	0.0294 mL	0.1469 mL	0.2938 mL	0.7345 mL

Keywords

E64FC26

2 Cited Publications

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E64FC26

Publications Citing Use of MedChemExpress (MCE) E64FC26

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

E64FC26 Related Classifications

HY-122895 Related Classifications