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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 | Availability | Quantity |
|---|---|---|---|
| 1 mg | $118 | In Stock | |
| 5 mg | $297 | 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: 90.0 mg/mL (194.9 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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