2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. APE1-IN-1

APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells.

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

APE1-IN-1 Chemical Structure

APE1-IN-1 Chemical Structure

CAS No. : 524708-03-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 137 In-stock
Solution
10 mM * 1 mL in DMSO USD 137 In-stock
Solid
5 mg USD 125 In-stock
10 mg USD 200 In-stock
50 mg USD 600 In-stock
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Based on 1 publication(s) in Google Scholar

APE1-IN-1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells[1].

IC50 & Target

IC50: 2 μM (APE1)[1]
In Vitro

APE1-IN-1 (compound 3) exhibits an IC50 of 2 μM in the qHTS assay and an IC50 of 12 μM in a radiotracer incision assay (RIA)[1].
APE1-IN-1 (0, 1, 3, 10, 30, or 100 μM; 15 min) inhibits HeLa whole cell extract AP site incision in a dose-dependent manner[1].
APE1-IN-1 (5-30 μM; 24 h) exhibits cytotoxic activity against HeLa cells, and potentiates the activity of methyl methansulfonate and Temozolomide (HY-17364)[1].

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

APE1-IN-1 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HeLa cells
Concentration: 5-30 μM
Incubation Time: 24 h
Result: Exhibited cytotoxic activity against HeLa cells with a 50% reduction in cell viability occurring at ~15 μM.
Greatly potentiated the activity of methyl methansulfonate (0.4 mM) and Temozolomide (HY-17364) (1 mM) with optimal synergy occurring at ~5 μM and ~10 μM, respectively.
In Vivo

APE1-IN-1 (30 mpk; IP; single dosage) exhibits favorable pharmacokinetic property[1].
Pharmacokinetic Parameters of APE1-IN-1 (compound 3) (IP; 30 mpk) in CD1 mice[1].

Plasma Brain
t1/2 (h) 2.1 1
brain/plasma 21
Cmax (μM) 16 217
tmax (h) 0.25 0.25
CLogP 2.83

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

Animal Model: CD1 male mice (n = 3)[1]
Dosage: 30 mpk
Administration: IP; single dosage
Result: Showed lipophilic (CLogP = 2.8), crossed the BBB quite readily, giving rise to a B/P ratio of 21.
Molecular Weight

371.52

Formula

C19H21N3OS2
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CC(NC(S1)=C(C2=NC3=CC=CC=C3S2)C4=C1CN(C(C)C)CC4)=O
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 : 22 mg/mL (59.22 mM; ultrasonic and warming and heat to 80°C; 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 2.6916 mL 13.4582 mL 26.9165 mL
5 mM 0.5383 mL 2.6916 mL 5.3833 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
=
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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  Corn Oil

    Solubility: 5 mg/mL (13.46 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  50% PEG300    50% Saline

    Solubility: 2.5 mg/mL (6.73 mM); Suspended solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥99.0%

COA (255 KB) Elemental Analysis Report (113 KB)

Handling Instructions (2659 KB)
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 2.6916 mL 13.4582 mL 26.9165 mL 67.2911 mL
5 mM 0.5383 mL 2.6916 mL 5.3833 mL 13.4582 mL
10 mM 0.2692 mL 1.3458 mL 2.6916 mL 6.7291 mL
15 mM 0.1794 mL 0.8972 mL 1.7944 mL 4.4861 mL
20 mM 0.1346 mL 0.6729 mL 1.3458 mL 3.3646 mL
25 mM 0.1077 mL 0.5383 mL 1.0767 mL 2.6916 mL
30 mM 0.0897 mL 0.4486 mL 0.8972 mL 2.2430 mL
40 mM 0.0673 mL 0.3365 mL 0.6729 mL 1.6823 mL
50 mM 0.0538 mL 0.2692 mL 0.5383 mL 1.3458 mL
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APE1-IN-1 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:

APE1-IN-1524708-03-0DNA/RNA SynthesisanticancerTemozolomideHeLaCD1BBBInhibitorinhibitorinhibit

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