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ART812 is an orally active inhibitor of DNA polymerase Polθ, possessing an IC50 value of 7.6 nM. Additionally, ART812 exhibits a cell-based microhomology-mediated end joining (MMEJ) IC50 value of 240 nM.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $118 | - | In Stock | |
| 5 mg | $297 | In Stock | In Stock | |
| 10 mg | $475 | - | In Stock | |
| 25 mg | $786 | - | In Stock | |
| 50 mg | $1,160 | - | In Stock | |
| 100 mg | $1,620 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $295 | - | In Stock |
| Description | ART812 is an orally active inhibitor of DNA polymerase Polθ, possessing an IC50 value of 7.6 nM. Additionally, ART812 exhibits a cell-based microhomology-mediated end joining (MMEJ) IC50 value of 240 nM. |
| Targets&IC50 | Polymerase θ:7.6 nM (IC50) |
| In vitro | ART812 (0-40 μM) induces Polθ inhibitor sensitivity in MDA-MB-436 SHLD2 knockout cells [1]. |
| In vivo | ART812 (100?mg/kg; p.o. daily for 76 days) shows significant tumour inhibition in rats bearing established MDA-MB-436 BRCA1/SHLD2 defective tumours (volume 250-350?mm 3 ) [1] . |
| Synonyms | ART812 |
| Molecular Weight | 461.79 |
| Formula | C19H16ClF4N3O4 |
| Cas No. | 2607138-82-7 |
| Smiles | CN(C(=O)[C@@H]1[C@H](O)[C@H](O)C(=O)N1c1cc(cc(C)n1)C(F)(F)F)c1ccc(F)c(Cl)c1 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 90 mg/mL (194.89 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.15 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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