2. Immunology/Inflammation PI3K/Akt/mTOR Cell Cycle/DNA Damage
  3. FLAP ATM/ATR
  4. FEN1-IN-1

FEN1-IN-1 (compound 1) is a small molecule flap endonuclease 1 (FEN1) inhibitor with antitumor activity. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg2+ ions. FEN1-IN-1 initiaties a DNA damage response and activates the ATM checkpoint signalling pathway, the phosphorylation of histone H2AX and the ubiquitination of FANCD2 in mammalian cells. FEN1-IN-1 is promising for research of cancers.

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

FEN1-IN-1 Chemical Structure

FEN1-IN-1 Chemical Structure

CAS No. : 824983-91-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
1 mg USD 28 In-stock
5 mg USD 60 In-stock
10 mg USD 90 In-stock
50 mg USD 190 In-stock
100 mg USD 290 In-stock
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Based on 4 publication(s) in Google Scholar

FEN1-IN-1 Related Antibodies

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Description

FEN1-IN-1 (compound 1) is a small molecule flap endonuclease 1 (FEN1) inhibitor with antitumor activity. FEN1-IN-1 binds to the active site of FEN1 and partly achieves inhibition by the co-ordination of Mg2+ ions. FEN1-IN-1 initiaties a DNA damage response and activates the ATM checkpoint signalling pathway, the phosphorylation of histone H2AX and the ubiquitination of FANCD2 in mammalian cells. FEN1-IN-1 is promising for research of cancers[1].

IC50 & Target

FEN1[1]
In Vitro

FEN1-IN-1 (0-30 μM, 3 days) inhibits 212 cell-lines growth with a mean GI 50 of 15.5 μM[1].
FEN1-IN-1 (0.2-20 μM, 24 h) induces Hela cells disrupted for MRE11A more sensitive and decreasea the survival of the MRE11A deficient cell-lines due to cytotoxicity[1].
FEN1-IN-1 (0-10 μM, 24 h) inhibits both FEN1 and EXO1 function and induces a DNA damage response to activate the signalling pathways in SW620 and HCT-116 cells[1].
FEN1-IN-1 (10 μM, 24 h) leads to replication fork instabilities that, if left unrepaired, can lead to cell death[1].

Tissue-specific sensitivity to FEN1-IN-1 (GI50: μM)[1]

FEN1-IN-1 Bladder Breast Colorectal Gastric Liver Lung Pancreatic Prostate Gynae Head & Neck
Cell-lines screened 19 22 21 25 21 37- 24 7 21 15

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

FEN1-IN-1 Related Antibodies
Molecular Weight

332.33

Formula

C15H12N2O5S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(CC2OC3=CC=CC=C3OC2)C(C=CS4)=C4C(N1O)=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 : 250 mg/mL (752.26 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 3.0091 mL 15.0453 mL 30.0906 mL
5 mM 0.6018 mL 3.0091 mL 6.0181 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 (6.26 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 (6.26 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 3.0091 mL 15.0453 mL 30.0906 mL 75.2264 mL
5 mM 0.6018 mL 3.0091 mL 6.0181 mL 15.0453 mL
10 mM 0.3009 mL 1.5045 mL 3.0091 mL 7.5226 mL
15 mM 0.2006 mL 1.0030 mL 2.0060 mL 5.0151 mL
20 mM 0.1505 mL 0.7523 mL 1.5045 mL 3.7613 mL
25 mM 0.1204 mL 0.6018 mL 1.2036 mL 3.0091 mL
30 mM 0.1003 mL 0.5015 mL 1.0030 mL 2.5075 mL
40 mM 0.0752 mL 0.3761 mL 0.7523 mL 1.8807 mL
50 mM 0.0602 mL 0.3009 mL 0.6018 mL 1.5045 mL
60 mM 0.0502 mL 0.2508 mL 0.5015 mL 1.2538 mL
80 mM 0.0376 mL 0.1881 mL 0.3761 mL 0.9403 mL
100 mM 0.0301 mL 0.1505 mL 0.3009 mL 0.7523 mL
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FEN1-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:

FEN1-IN-1824983-91-7FLAPATM/ATR5-lipoxygenase-activating protein5-LO activating proteinAtaxia telangiectasia mutatedATM and RAD3 relatedFEN1Mg2+ ionsDNA damage responseATM checkpoint signalling pathwayH2AXFANCD2mammalian cellscancersInhibitorinhibitorinhibit

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