Antitumor agent-53

Antitumor agent-53 is a potent antitumor agent. Antitumor agent-53 induces cell cycle arrest at the G2/M phase. Antitumor agent-53 inhibits the PI3K/AKT pathway to induce the apoptosis of HGC-27 cells. Antitumor agent-53 has the potential for the research of gastrointestinal tumors[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Antitumor agent-53 (compound 6f) (0, 0.22, 0.67, 2, 6, 18 µM; 72 h) shows anti-proliferation activity with IC50s of 3.10, 0.37, 4.01, >18, 7.87, 9.11 µM for HGC-27, HT-29, HepG-2, A549, MCF7, GES-1 cells[1]. Antitumor agent-53 (0.15, 0.3, 0.6 µM) shows anti-proliferative activity in HGC-27 and HT-29 cells with a dose-dependent manner[1]. Antitumor agent-53 (100, 200 µM) shows a certain inhibitory activity against Topo I at 200 μM[1]. Antitumor agent-53 (0.1, 0.3, 0.9 μM; 24 h) induces cell cycle arrest at the G2/M phase in HGC-27, HT-29 cells[1]. Antitumor agent-53 (0.1, 0.3, 0.9, 2.7 μM; 24 h) induces the apoptosis of HGC-27 and HT-29 cells in a concentration-dependent manner[1]. Antitumor agent-53 (0.15, 0.3, 0.6 μM; 24 h) inhibits the migration and invasion of HGC-27 cells in a concentration-dependent manner[1]. Antitumor agent-53 (0.1, 0.3, 0.9 μM; 24 h) suppresses the PI3K/AKT pathway to induce the apoptosis of HGC-27 cells[1]. Cell Proliferation Assay[1] Cell Line: HGC-27, HT-29, HepG-2, A549, MCF7, GES-1 cells Concentration: 0, 0.22, 0.67, 2, 6, 18 µM Incubation Time: 72 h Result: Showed anti-proliferation activity with IC50s of 3.10, 0.37, 4.01, >18, 7.87, 9.11 µM for HGC-27, HT-29, HepG-2, A549, MCF7, GES-1 cells. Cell Cycle Analysis[1] Cell Line: HGC-27, HT-29 cells Concentration: 0.1, 0.3, 0.9 μM Incubation Time: 24 h Result: Cells were arrest at the G2/M phase. Apoptosis Analysis[1] Cell Line: HGC-27, HT-29 cells Concentration: 0.1, 0.3, 0.9, 2.7 μM Incubation Time: 24 h Result: Induced the apoptosis of HGC-27 and HT-29 cells in a concentration-dependent manner. Western Blot Analysis[1] Cell Line: HGC-27 cells Concentration: 0.1, 0.3, 0.9 μM Incubation Time: 24 h Result: Suppressed the PI3K/AKT pathway to induce the apoptosis of HGC-27 cells.

[1]. Hao X, et al. Design, synthesis and bioactivity evaluation of novel N-phenyl-substituted evodiamine derivatives as potent anti-tumor agents. Bioorg Med Chem. 2021; 55:116595.