2. Cell Cycle/DNA Damage NF-κB Immunology/Inflammation Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK
  3. DNA/RNA Synthesis NF-κB AP-1 HIF/HIF Prolyl-Hydroxylase VEGFR Reactive Oxygen Species
  4. E3330

E3330 (APX-3330) is a direct, orally active and selective inhibitor of Ape-1 (apurinic/apyrimidinic endonuclease 1)/Ref-1 (redox factor-1) redox. E3330 is able to impair tumor growth and blocks the activity of NF-κB, AP-1, and HIF-1α in pancreatic cancer. E3330 shows anticancer activities.

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E3330 Chemical Structure

E3330 Chemical Structure

CAS No. : 136164-66-4

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10 mM * 1 mL in DMSO
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Based on 3 publication(s) in Google Scholar

E3330 Related Antibodies

Top Publications Citing Use of Products

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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c-Fos c-Jun

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HIF-1α HIF

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

E3330 (APX-3330) is a direct, orally active and selective inhibitor of Ape-1 (apurinic/apyrimidinic endonuclease 1)/Ref-1 (redox factor-1) redox. E3330 is able to impair tumor growth and blocks the activity of NF-κB, AP-1, and HIF-1α in pancreatic cancer. E3330 shows anticancer activities[1][2][3][4][5].

IC50 & Target

Ape-1, Ref-1[1]
In Vitro

E3330 (0-50 μM, 48 h) inhibits the growth of HUVECs, PCECs and EPCs[1].
E3330 (0-5 μM) reduces secreted and intracellular VEGF (vascular endothelial growth factor) expression by pancreatic cancer cells, while concomitantly downregulating the cognate receptor Flk-1/KDR on PCECs[1].
E3330 (0-1 μM) inhibits the differentiation of bone marrow mesenchymal stem cells (BM-MSCs) into CD31+ cells of endothelial lineage[1].
E3330 (0-50 μM, 72 h) decreases cell viability in H1975 cells about 45% at 50 μM[2].
E3330 (0-30 μM) inhibits the growth and migration of pancreatic cancer cells[3].
E3330 (0-30 μM) significantly enhances intracellular ROS level and inhibits CD44 expression in PANC1 cells[3].

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

E3330 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Human umbilical vein endothelial cells (HUVECs), murine pancreatic cancer associated endothelial cells (mPCECs), human endothelial progenitor cells (hEPCs)
Concentration: 1, 5, and 10 μM (HUVECs); 1. 5, 10. 20. 30, 40, and 50 μM (mPCECs); 1, 5, 10, 15, 20, 25, and 30 μM (hEPCs)
Incubation Time: 48 h
Result: Inhibited the growth of HUVECs, PCECs and EPCs.

Western Blot Analysis[1]

Cell Line: mPCECs
Concentration: 1, 5, and 10 μM
Incubation Time: 48 h
Result: Inhibited the growth of HUVECs, PCECs and EPCs.

Cell Viability Assay[2]

Cell Line: H1975 cells
Concentration: 0, 5, 10, 20, 30, 40, and 50 μM
Incubation Time: 72 h
Result: Showed decreased cell viability in about 45% at 50 µM.
In Vivo

E3330 (25 mg/kg, Orally, 5 daily, five days each week for three weeks) is neuroprotective against cisplatin-induced alterations in capsaicin-induced vasodilation[4].
E3330 (0-100 mg/kg, Orally, once) attenuates the liver injury when given at 1 h, 6 h or 12 h after galactosamine challenge[5].

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

Animal Model: Sprague-Dawley rats (adult male, 150-175 g)[4]
Dosage: 25 mg/kg
Administration: Orally, 5 daily, five days each week for three weeks
Result: Attenuated the cisplatin-induced decrease in capsaicin-induced vasodilatation in the rat hindpaw.
Animal Model: Male Fischer (F344/DuCrj) rats (160-190 g)[5]
Dosage: 0, 10, 30, and 100 mg/kg
Administration: Orally, 1 h, 6 h or 12 h after galactosamine challenge
Result: Attenuated the liver injury when given at 1 h, 6 h or 12 h after galactosamine challenge.
Clinical Trial
Molecular Weight

378.46

Formula

C21H30O6
CAS No.
Appearance

Solid

Color

Yellow to orange

SMILES

CCCCCCCCC/C(C(O)=O)=C\C1=C(C)C(C(OC)=C(OC)C1=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 120 mg/mL (317.07 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 2.6423 mL 13.2114 mL 26.4229 mL
5 mM 0.5285 mL 2.6423 mL 5.2846 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (5.50 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6423 mL 13.2114 mL 26.4229 mL 66.0572 mL
5 mM 0.5285 mL 2.6423 mL 5.2846 mL 13.2114 mL
10 mM 0.2642 mL 1.3211 mL 2.6423 mL 6.6057 mL
15 mM 0.1762 mL 0.8808 mL 1.7615 mL 4.4038 mL
20 mM 0.1321 mL 0.6606 mL 1.3211 mL 3.3029 mL
25 mM 0.1057 mL 0.5285 mL 1.0569 mL 2.6423 mL
30 mM 0.0881 mL 0.4404 mL 0.8808 mL 2.2019 mL
40 mM 0.0661 mL 0.3303 mL 0.6606 mL 1.6514 mL
50 mM 0.0528 mL 0.2642 mL 0.5285 mL 1.3211 mL
60 mM 0.0440 mL 0.2202 mL 0.4404 mL 1.1010 mL
80 mM 0.0330 mL 0.1651 mL 0.3303 mL 0.8257 mL
100 mM 0.0264 mL 0.1321 mL 0.2642 mL 0.6606 mL
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E3330 Related Classifications

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.

Keywords:

E3330136164-66-4APX-3330E 3330E-3330APX3330APX 3330DNA/RNA SynthesisNF-κBAP-1HIF/HIF Prolyl-HydroxylaseVEGFRReactive Oxygen SpeciesNuclear factor-κBNuclear factor-kappaBActivator Protein 1Hypoxia-inducible factorsHIFsHIF-PHVascular endothelial growth factor receptorH1975PANC1HUVECsPCECsEPCsorallyAPendonuclease1APE1REF-1DNA-bindingTNF-αIL-8NSCLC cellsanticancerpancreatic cancerneuroprotectiveInhibitorinhibitorinhibit

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