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Chemical Structure : ART899
Catalog No.: PC-49680Not For Human Use, Lab Use Only.
ART899 (ART-899) is a potent, specific allosteric inhibitor of DNA polymerase theta (Polθ), specifically inhibits Polθ MMEJ activity with IC50 of 180 nM, shows with improved in vivo stability compared to ART558.
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ART899 (ART-899) is a potent, specific allosteric inhibitor of DNA polymerase theta (Polθ), specifically inhibits Polθ MMEJ activity with IC50 of 180 nM, shows with improved in vivo stability compared to ART558.
ART899 effectively radiosensitizes HCT116 and H460 cells at both 1 µM and 3 µM.
ART899 specifically radiosensitizes tumor cells with no effect on some non-cancerous cells.
The combination of Polθ inhibition using ART899 with fractionated radiation is well tolerated and results in a significant reduction in tumor growth compared to radiation alone.
| M.Wt | 463.83 | |
| Formula | C20H14D3ClF4N2O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Gonzalo Rodriguez-Berriguete, et al. Clin Cancer Res. 2023 Jan 23;CCR-22-2977.
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