A011, a potent and selective ataxia-telangiectasia mutated (ATM) inhibitor, exhibits an IC50 of 1.0 nM and triggers apoptosis as well as G2/M phase cell cycle arrest when combined with CPT-11, displaying notable antitumor activity [1].

Compound A011 (compound 8d) at concentrations of 10, 30, and 100 nM applied for 5 days increases the sensitivity of SW620 and HCT116 cells to CPT-11 (100 nM) [1]. When administered in conjunction with CPT-11 at doses ranging from 0 to 100 nM for 24 and 72 hours, A011 induces apoptosis and cell cycle arrest at the G2/M phase [1]. Furthermore, A011 at concentrations of 3, 9, 27, 83, and 250 nM reduces the expression of p-ATM and p-Chk2 in a dose-dependent manner in SW620 cells under irradiation conditions of 1.5 or 3 Gy [1].

A011 (5 mg/kg; intraperitoneal injection; daily for 23 days) combined with CPT-11 (5 mg/kg, intraperitoneal injection; once weekly) demonstrated antitumor activity in mice [1].