Anticancer agent 53

Anticancer agent 53 is a potent anticancer agent. Anticancer agent 53 shows in vitro cytotoxicity. Anticancer agent 53 induces apoptosis and cell cycle arrest in S/G2/M phases. Anticancer agent 53 shows antitumor activity with no apparent toxicity[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Anticancer agent 53 (compound c20) (0-1000 nM; 72 h) shows cytotoxicity with IC50s of 2.3, 42.0, 4.3, 96.3, 24.0, 47.4 nM for Hep3B, MCF7, A549, MDA-MB-231, KB, KB-vin cells, respectively[1]. Anticancer agent 53 (0.025, 0.05, 0.1 µM; 48 h) induces apoptosis and cell cycle arrest in S/G2/M phases[1]. Anticancer agent 53 (0.1. 0.2 µM; 6 h) inhibits topoisomerase I activity in A549 cells[1]. Cell Cycle Analysis[1] Cell Line: A549 cells Concentration: 0.025, 0.05, 0.1 µM Incubation Time: 0-48 h Result: Induced cell cycle arrest in S/G2/M phases. Apoptosis Analysis[1] Cell Line: A549 cells Concentration: 0.025, 0.05, 0.1 µM Incubation Time: 0-48 h Result: Induced apoptosis with the proapoptotic protein Caspase-3 and Bax were up-regulated and anti-apoptotic Bcl-2 was down-regulated.

Anticancer agent 53 (5, 25 and 50 mg/kg; IP) shows no apparent toxicity to mouse liver, kidney and hemopoietic system[1]. Anticancer agent 53 (2 mg/kg; i.v; every other day for two weeks) shows antitumor effect in HCC mouse model[1]. Animal Model: Balb/C mice[1] Dosage: 5, 25 and 50 mg/kg (saline with 5% DMSO and 5% Cremophor EL) Administration: I.p. Result: Showed no body weight loss, no significant liver damage, no significant damage occurred in spleens and livers. Animal Model: 6-8 weeks Female BALB/c nude mice (Hep3B cells)[1] Dosage: 1, 2 mg/kg Administration: I.v., every other day for total 7 doses Result: Significantly inhibited tumor growth with an average body weight of 24 g and an average tumor volume of 3800 mm[3] at 1 mg/kg and an average body weight of 22 g and average tumor volume 2380 mm[3] at 2 mg/kg. Animal Model: 6-8 weeks FVB/N mice (HCC mouse model)[1] Dosage: 2 mg/kg Administration: I.v.; every other day for two weeks Result: Inhibited the tumor growth and reduced the liver weights, and t inhibited proliferation of HCC tissues.

[1]. Yang CJ, et al. Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin. Eur J Med Chem. 2020 Feb 1;187:111971.