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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 | $233 | In Stock | |
5 mg | $575 | In Stock | |
10 mg | $892 | In Stock | |
25 mg | $1,550 | In Stock | |
50 mg | $1,980 | In Stock | |
100 mg | $2,660 | In Stock | |
1 mL x 10 mM (in DMSO) | $659 | 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] . |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 90.0 mg/mL (194.9 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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