In Vitro: A011 (compound 8d) (10, 30, 100 nM; 5 days) increases the sensitivity of SW620 and HCT116 cells to CPT-11 (HY-16562) (100 nM). A011 (0-100 nM; 24, 72 h) induces apoptosis and cell cycle arrest at G2/M phase when combinanted with CPT-11. A011 (3, 9, 27, 83, 250 nM) decreases the expression of p-ATM and p-Chk2 in a dose-dependent manner under 1.5 or 3 Gy irradiation conditions in SW620 cells.
In Vivo: A011 (5 mg/kg; i.p.; once daily for 23 days) combines with CPT-11 (5 mg/kg, i.p.; once a week) shows antitumor activity in mice.