1. Apoptosis Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  2. Apoptosis PDI
  3. E64FC26

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.

For research use only. We do not sell to patients.

E64FC26 Chemical Structure

E64FC26 Chemical Structure

CAS No. : 2285446-62-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 550 In-stock
Solution
10 mM * 1 mL in DMSO USD 550 In-stock
Solid
1 mg USD 200 In-stock
5 mg USD 500 In-stock
10 mg USD 850 In-stock
25 mg USD 1800 In-stock
50 mg USD 3000 In-stock
100 mg USD 4600 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of E64FC26:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

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 (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.
Molecular Weight

340.39

Formula

C19H23F3O2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9378 mL 14.6890 mL 29.3781 mL
5 mM 0.5876 mL 2.9378 mL 5.8756 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

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.

  • 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.

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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E64FC26
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