TX-2552 is an orally active tyrosine DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 value of 0.62 μM. TX-2552 can enhance the clastogenic activity of Topotecan in mouse bone marrow cells, as well as the anti-tumor effect of Topotecan in Krebs-2 ascites tumor mice.
TX-2552 (20-160 mg/kg; p.o.) can enhance the clastogenic effects of Topotecan in mice with chromosomal abnormalities in bone marrow cells[1].TX-2552 (20-120 mg/kg; once daily; 18 days; i.p.) can enhance the anti-tumor effect of topotecan in Krebs-2 ascites tumor mice[2].
References:
[1]. Zhanataev AK, et al. Enhancement of the Clastogenic Effects of Topotecan In Vivo by Tyrosyl-DNA Phosphodiesterase 1 Inhibitors. Bull Exp Biol Med. 2024 May;177(1):30-34.
[2]. Khomenko TM, et al. Promising New Inhibitors of Tyrosyl-DNA Phosphodiesterase I (Tdp 1) Combining 4-Arylcoumarin and Monoterpenoid Moieties as Components of Complex Antitumor Therapy. Int J Mol Sci. 2019 Dec 23;21(1):126.