ART812
Based on 3 publication(s) in Google Scholar
ART812 is an orally active DNA polymerase Polθ inhibitor with an IC50 value of 7.6 nM. ART812 has an IC50 value of 240 nM for cell based microhomology-mediated end joining (MMEJ).
For research use only. We do not sell to patients.
- Purity: 99.90%
- CAS No.: 2607138-82-7
- Formula: C19H16ClF4N3O4
- Molecular Weight:461.79
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
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Anti-Cancer Compound Library
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Publications Citing Use of MedChemExpress (MCE) ART812
MoreAll DNA/RNA Synthesis Isoforms
More
Biological Activity
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DNA Polymerase |
Polθ 7.6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| DLD-1 | EC50 |
>12 μM
Compound: 43; ART812
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Antiproliferative activity against human DLD-1 cells
Antiproliferative activity against human DLD-1 cells
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[PMID: 36200480] |
| DLD-1 | EC50 |
1.1 μM
Compound: 43; ART812
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Antiproliferative activity against human BRCA-2 deficient DLD-1 cells
Antiproliferative activity against human BRCA-2 deficient DLD-1 cells
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[PMID: 36200480] |
| HEK293 | EC50 |
240 nM
Compound: 43; ART812
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Inhibition of microhomology-mediated end joining in HEK293 cells
Inhibition of microhomology-mediated end joining in HEK293 cells
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[PMID: 36200480] |
ART812 (0-40 μM) elicits Polθ inhibitor sensitivity in MDA-MB-436 SHLD2 knockout cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2607138-82-7
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Appearance Solid
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Molecular Weight 461.79
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Formula C19H16ClF4N3O4
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Color White to yellow
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SMILES
O=C([C@H]([C@H](O)[C@@H]1O)N(C2=NC(C)=CC(C(F)(F)F)=C2)C1=O)N(C3=CC=C(F)C(Cl)=C3)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
2026 Mar 17;7(3):102687. PMID: 41850232 -
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bioRxiv
DNA polymerase theta-mediated DNA repair is a functional dependency and therapeutic vulnerability in DNMT3A deficient leukemia cells. [Abstract]2024 Sep 19:2024.09.15.613155. PMID: 39411165
Solvent & Solubility
DMSO : 100 mg/mL (216.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.41 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.41 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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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 | 2.1655 mL | 10.8274 mL | 21.6549 mL | 54.1372 mL |
| 5 mM | 0.4331 mL | 2.1655 mL | 4.3310 mL | 10.8274 mL | |
| 10 mM | 0.2165 mL | 1.0827 mL | 2.1655 mL | 5.4137 mL | |
| 15 mM | 0.1444 mL | 0.7218 mL | 1.4437 mL | 3.6091 mL | |
| 20 mM | 0.1083 mL | 0.5414 mL | 1.0827 mL | 2.7069 mL | |
| 25 mM | 0.0866 mL | 0.4331 mL | 0.8662 mL | 2.1655 mL | |
| 30 mM | 0.0722 mL | 0.3609 mL | 0.7218 mL | 1.8046 mL | |
| 40 mM | 0.0541 mL | 0.2707 mL | 0.5414 mL | 1.3534 mL | |
| 50 mM | 0.0433 mL | 0.2165 mL | 0.4331 mL | 1.0827 mL | |
| 60 mM | 0.0361 mL | 0.1805 mL | 0.3609 mL | 0.9023 mL | |
| 80 mM | 0.0271 mL | 0.1353 mL | 0.2707 mL | 0.6767 mL | |
| 100 mM | 0.0217 mL | 0.1083 mL | 0.2165 mL | 0.5414 mL |
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