RTx-303 | DNA Polθ inhibitor | Probechem Biochemicals

Chemical Structure : RTx-303

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RTx-303 (RTx303)

货号: PC-25710Not For Human Use, Lab Use Only.

RTx-303 is a potent, selective, allosteric and orally active inhibitor of DNA polymerase θ (Polθ) with IC50 of 5.8 nM, shows no significant inhibition of other eukaryotic DNA polymerases, including the related A-family Polγ.

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生物&药学活性

RTx-303 is a potent, selective, allosteric and orally active inhibitor of DNA polymerase θ (Polθ) with IC50 of 5.8 nM, shows no significant inhibition of other eukaryotic DNA polymerases, including the related A-family Polγ.
RTx-303 also shows no significant inhibition against a kinase panel.
RTx-303 exhibits significantly lower IC50 in HCT116 BRCA2–/– cells (IC50=81.2 nM) compared to Polθ-pol inhibitors RP-6685, ART558 and ART812 which bind to the same allosteric pocket.
RTx-303 exhibits selective killing of HRD cells in multiple cell lines.
RTx-303 potentiates PARPi in BRCA mutant cells and xenografts.

物理化学性质&存储条件

分子量	568.51
分子式	C25H23D3F7N3O4
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	2-(3-((R)-3-(dimethylamino)-2-hydroxypropyl)-2-oxoimidazolidin-1-yl)-4,6-bis(trifluoromethyl)phenyl 2-(4-fluorophenyl)propanoate-3,3,3-d3

参考文献

1. Chandramouly G, et al. J Med Chem. 2025 Oct 22. doi: 10.1021/acs.jmedchem.5c00551.

RTx-303 (RTx303)

生物&药学活性

物理化学性质&存储条件

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RTx-303 (RTx303)

生物&药学活性

物理化学性质&存储条件

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