XRD-0394 is a highly potent and orally active inhibitor of ATM and DNA-PKcs, exhibiting IC50 values of 0.39 nM and 0.89 nM, respectively. This compound demonstrates selectivity for its target enzymes over other members of the PIKK and PI3K families. In preclinical studies, XRD-0394 has been shown to significantly enhance the cytotoxic effects of ionizing radiation on tumor cells both in vitro and in vivo. Additionally, it can synergize with PARP and topoisomerase I inhibitors, making it a valuable tool for research in cancer treatment and DNA repair mechanisms.
XRD-0394 is a highly potent and orally active inhibitor of ATM and DNA-PKcs, exhibiting IC50 values of 0.39 nM and 0.89 nM, respectively. This compound demonstrates selectivity for its target enzymes over other members of the PIKK and PI3K families. In preclinical studies, XRD-0394 has been shown to significantly enhance the cytotoxic effects of ionizing radiation on tumor cells both in vitro and in vivo. Additionally, it can synergize with PARP and topoisomerase I inhibitors, making it a valuable tool for research in cancer treatment and DNA repair mechanisms.
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