2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. ART899

ART899 is a highly specific allosteric inhibitor of the Polθ DNA polymerase domain. ART899 can effectively enhance the radiosensitivity of tumor cells, shows good tolerance when combined with fractionated radiation, and significantly reduces tumor growth compared to radiation alone.

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

ART899

ART899 Chemical Structure

CAS No. : 2607139-85-3

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of ART899:

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

ART899 is a highly specific allosteric inhibitor of the Polθ DNA polymerase domain. ART899 can effectively enhance the radiosensitivity of tumor cells, shows good tolerance when combined with fractionated radiation, and significantly reduces tumor growth compared to radiation alone[1].

Application

1. This compound can be used as a tracer.
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.

IC50 & Target

DNA Polymerase

 

Molecular Weight

464.81

Formula

C19H13D3ClF4N3O4
CAS No.
Unlabeled CAS
Appearance

Solid

Color

White to off-white

SMILES

[2H]C([2H])([2H])N(C1=CC(Cl)=C(C=C1)F)C([C@H]2N(C3=CC(C(F)(F)F)=CC(C)=N3)C([C@H]([C@H]2O)O)=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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (215.14 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 2.1514 mL 10.7571 mL 21.5142 mL
5 mM 0.4303 mL 2.1514 mL 4.3028 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:

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: ≥ 2.5 mg/mL (5.38 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 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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 2.1514 mL 10.7571 mL 21.5142 mL 53.7854 mL
5 mM 0.4303 mL 2.1514 mL 4.3028 mL 10.7571 mL
10 mM 0.2151 mL 1.0757 mL 2.1514 mL 5.3785 mL
15 mM 0.1434 mL 0.7171 mL 1.4343 mL 3.5857 mL
20 mM 0.1076 mL 0.5379 mL 1.0757 mL 2.6893 mL
25 mM 0.0861 mL 0.4303 mL 0.8606 mL 2.1514 mL
30 mM 0.0717 mL 0.3586 mL 0.7171 mL 1.7928 mL
40 mM 0.0538 mL 0.2689 mL 0.5379 mL 1.3446 mL
50 mM 0.0430 mL 0.2151 mL 0.4303 mL 1.0757 mL
60 mM 0.0359 mL 0.1793 mL 0.3586 mL 0.8964 mL
80 mM 0.0269 mL 0.1345 mL 0.2689 mL 0.6723 mL
100 mM 0.0215 mL 0.1076 mL 0.2151 mL 0.5379 mL
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ART899 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:

ART8992607139-85-3ART 899ART-899DNA/RNA SynthesisInhibitorinhibitorinhibit

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