gartisertib

Gartisertib (M4344, also known as VX-803) is an orally available small molecule inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase. It acts as a highly potent and selective ATP-competitive inhibitor of ATR with a Ki of less than 150 pM. Gartisertib disrupts the ATR signaling pathway by inhibiting phosphorylation of checkpoint kinase 1 (Chk1), leading to increased DNA damage and cellular catastrophe in cancer cells. The drug demonstrates strong synergy with various DNA-damaging anticancer agents such as topoisomerase inhibitors (topotecan, irinotecan), gemcitabine, cisplatin, and talazoparib. Gartisertib is being developed primarily for the treatment of advanced solid tumors and has shown activity in preclinical models including patient-derived tumor organoids and xenografts[1][2][3][5][7].

Other names

gartisertibM4344M-4344M 4344VX-803VX803VX 803