tcsc7574 BAY-1895344 (hydrochloride)

BAY-1895344 hydrochloride is a potent, orally available and selective ATR inhibitor, with IC₅₀ of 7 nM.

IC50 & Target: IC50: 7 nM (ATR)^[2]

In Vitro: BAY-1895344 hydrochloride is a selective low-nanomolar inhibitor of ATR kinase activity, potently inhibiting proliferation of a broad spectrum of human tumor cell lines (median IC₅₀ of 78 nM). In cellular mechanistic assays BAY-1895344 inhibits hydroxyurea-induced H2AX phosphorylation demonstrating the anticipated mode of action^[1]. BAY-1895344 potently inhibits proliferation of a broad spectrum of human tumor cell lines (median IC₅₀=78 nM). In cellular mechanistic assays BAY-1895344 potently inhibits hydroxyurea-induced H2AX phosphorylation (IC₅₀=36 nM). Moreover, BAY-1895344 reveals significantly improved aqueous solubility, bioavailability across species and no activity in the hERG patch-clamp assay. BAY-1895344 also demonstrates very promising efficacy in monotherapy in DNA damage deficient tumor models as well as combination treatment with DNA damage inducing therapies^[2].

In Vivo: BAY-1895344 exhibits strong in vivo anti-tumor efficacy in monotherapy in a variety of xenograft models of different indications that are characterized by DDR deficiencies, inducing stable disease in ovarian and colorectal cancer or even complete tumor remission in mantle cell lymphoma models^[1].