ART899 | DNA Polθ inhibitor | Probechem Biochemicals

Chemical Structure : ART899

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ART899 (ART-899)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	463.83
分子式	C20H14D3ClF4N2O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(1S,2S,3S)-N-(3-chloro-4-fluorophenyl)-2,3-dihydroxy-N-(methyl-d3)-5-(6-methyl-4-(trifluoromethyl)pyridin-2-yl)-4-oxocyclopentane-1-carboxamide

参考文献

1. Gonzalo Rodriguez-Berriguete, et al. Clin Cancer Res. 2023 Jan 23;CCR-22-2977.

ART899 (ART-899)

生物&药学活性

物理化学性质&存储条件

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ART899 (ART-899)

生物&药学活性

物理化学性质&存储条件

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