Chemical Structure : RTx-303
CAS No.:
3035072-99-9
RTx-303
(RTx303)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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568.51
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Formula
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C25H23D3F7N3O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-(3-((R)-3-(dimethylamino)-2-hydroxypropyl)-2-oxoimidazolidin-1-yl)-4,6-bis(trifluoromethyl)phenyl 2-(4-fluorophenyl)propanoate-3,3,3-d3
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References
1. Chandramouly G, et al. J Med Chem. 2025 Oct 22. doi: 10.1021/acs.jmedchem.5c00551.
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