RP-6685

Description: RP-6685, a highly potent and selective inhibitor of DNA polymerase theta (Poltheta), manifests remarkable oral activity. With an IC 50 value of 5.8 nM in the PicoGreen assay, RP-6685 effectively hinders the enzymatic activity of Poltheta. In addition, it demonstrates significant antitumor efficacy as observed in a mouse tumor xenograft model [1]. Target: DNA/RNA Synthesis. Smiles: Nc1ccc(nn1)C#CCN(C(=O)Cc1ncc(cc1C(F)(F)F)C(F)(F)F)c1ccc(F)cc1. References: Bubenik M, et al. Identification of RP-6685, an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Poltheta. J Med Chem. 2022 Sep 20.