TP3011

TP3011 is a potent topoisomerase-1 inhibitor and is the active metabolite converted from TP3076 by aldehyde oxidase 1 (AOX1)[1]. TP3011 has robust anti-tumor activities against cancer cell lines[2].

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

Topoisomerase I

TP3011 (0-100 nM; 72 hours) inhibits cell proliferative activities against various human cancer cell lines, producing 50% inhibition (IC50) of cell growth of 0.85 nM; 8.5 nM; and 8.2 nM in HCT116, QG56, and NCI-H460 (NSCLC) cells, respectively[2]. Cell Proliferation Assay[2] Cell Line: HCT116, QG56, and NCI-H460 (NSCLC) cells Concentration: 0-100 nM Incubation Time: 72 hours Result: Was against human cancer cell lines, such as CRC and NSCLC cell lines.

[1]. Anthoney DA, et al. Phase I study of TP300 in patients with advanced solid tumors with pharmacokinetic, pharmacogenetic and pharmacodynamic analyses.BMC Cancer. 2012 Nov 21;12:536.

[2]. Niizuma S, et al. Synthesis of new camptothecin analogs with improved antitumor activities.Bioorg Med Chem Lett. 2009 Apr 1;19(7):2018-21.