(R,R)-ART0380 is a potent and selective ATR inhibitor for solid tumor research

**Background**

Ataxia telangiectasia and Rad3-related (ATR) kinase is a critical sensor of replication stress and DNA damage in eukaryotic cells. ATR plays a pivotal role in maintaining genomic stability by coordinating the DNA damage response (DDR), preventing premature entry into mitosis, and facilitating the repair of stalled replication forks. In many types of cancer, the ATR pathway is frequently upregulated to compensate for high levels of replication stress and genomic instability, allowing tumor cells to survive and resist conventional chemotherapy. Consequently, the inhibition of ATR has emerged as a promising therapeutic strategy to sensitize cancer cells to DNA-damaging agents and induce mitotic catastrophe. In this context, we will introduce a potent and selective ATR inhibitor – (R,R)-ART0380.

**Definition**

(R,R)-ART0380 is the enantiomer of ART0380 and serves as a highly potent and selective inhibitor of the ATR kinase. According to the (R,R)-ART0380 description, this compound is designed to target the ATR pathway to inhibit the growth of advanced or metastatic solid tumors.

**In Vitro and In Vivo Studies**

The chemical properties of this compound are defined by the (R,R)-ART0380 Formula C18H24N6O2S, with a molecular weight of 388.49. Regarding (R,R)-ART0380 biological activity, the parent compound ART0380 has demonstrated significant efficacy in targeting the ATR kinase, leading to the accumulation of DNA damage and subsequent cell death in various cancer models. Specifically, (R,R)-ART0380 in vitro studies focus on its ability to selectively inhibit ATR phosphorylation and downstream signaling pathways in cancer cell lines. Furthermore, (R,R)-ART0380 In Vivo research has highlighted its potential in treating advanced or metastatic solid tumors, where it disrupts the DNA repair mechanisms essential for tumor cell survival. These findings have supported the progression of the ART0380 series into Phase 2 clinical studies for the treatment of advanced or metastatic solid cancers. In conclusion, (R,R)-ART0380 is a potent and selective ATR inhibitor that holds significant promise for (R,R)-ART0380 Cancer research and the development of targeted therapies for solid tumors.

Keywords

(R,R)-ART0380, 2267316-75-4, Drug Isomer, solid tumors, Inhibitor, inhibitor, inhibit

References

[1] Carroll CL, et al. Discovery of ART0380, a Potent and Selective ATR Kinase Inhibitor Undergoing Phase 2 Clinical Studies for the Treatment of Advanced or Metastatic Solid Cancers. J Med Chem. 2024 Dec 26;67(24):21890-21904.