2-[2-(二乙氨基)乙基]-9-羟基-5,11-二甲基-6H-吡啶并[4,3-B]咔唑

Datelliptium (100 μM) shows significantly cytotoxic effects after 2 hr of treatment in suspension and primary cultures of rat hepatocytes. Datelliptium mobilizes glycogen in both rat systems in vitro concentration dependently. The half-maximal effect is 14.3 μM in isolated hepatocytes, whereas in cultured rat hepatocytes it is 5.9 μM. Datelliptium also leads to a concentration-dependent decrease in gluconeogenesis from lactate in cells. Datelliptium acetate is selectively cytotoxic for solid tumors over leukemia L1210. Human tumors H-125 and HCT-116 demonstrates less sensitivity to datelliptium acetate.

Upon intravenous administration, datelliptium acetate shows potent inhibitory activities in vivo against a variety of murine solid tumors. Datelliptium acetate is highly active against early-stage colon #38 with highest non-toxic dose (HNTD) of 170 mg/kg TD, and weight loss of 10%, T/C of 0%.