RTx-303

RTx-303 is an orally active, selective DNA polymerase θ (Polθ) inhibitor (IC50 = 5.1 nM) . RTx-303 exhibits significantly high cellular potency and strongly potentiates PARPi in BRCA1/2 mutant cells and patient-derived xenograft models. RTx-303 can be used for the study of BRCA2-mutated breast cancer[1].

Product Specifications

CAS Number

[3035072-99-9]

UNSPSC

12352005

Target

DNA/RNA Synthesis

Related Pathways

Cell Cycle/DNA Damage

Field of Research

Cancer

Smiles

CN(C)C[C@@H](O)CN(C1=O)CCN1C2=C(OC(N(C([2H])([2H])[2H])C3=CC=C(F)C=C3)=O)C(C(F)(F)F)=CC(C(F)(F)F)=C2

Molecular Formula

C24H22D3F7N4O4

Molecular Weight

569.49

References & Citations

[1]Chandramouly G, et al. RTx-303, an Orally Bioavailable Polθ Polymerase Inhibitor That Potentiates PARP Inhibitors in BRCA Mutant Tumors. J Med Chem. 2025 Nov 13;68 (21) :22196-22215.