E64FC26
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.48%
- No. CAS: 2285446-62-8
- Fòrmula: C19H23F3O2
- Peso molecular:340.39
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) E64FC26
More
Actividad biológica
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 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.
? 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].
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
-
No. CAS 2285446-62-8
-
Appearance Solid
-
Peso molecular 340.39
-
Fòrmula C19H23F3O2
-
Color Light yellow to yellow
-
SMILES
OC1=CC2=C(/C(C=C2C(F)(F)F)=C/CCCCCCCC)C=C1O.[(E)]
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
-
Journal Impact Factor
-
Most Recent
-
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
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (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)
-
Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
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.
| 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 |
E64FC26 Related Classifications
HY-122895 Related Classifications
Powered by Bioz