PNU-159682 is a major bioactive metabolite of Nemorubicin in human liver microsomes; > 3,000-fold cytotoxic than its parent compound(MMDX and doxorubicin).

IC50 value: 0.1-0.5 nM (HT-29; DU145; Jurkat cell lines, etc) [1]

Target: Topoisomerase I inhibitor

in vitro: The cytotoxicity of PNU-159682 were in the subnanomolar range (0.07-0.58 nmol/L) and noticeably lower than that recorded for both MMDX and doxorubicin; PNU-159682 was 2,360- to 790-fold and 6,420- to 2,100-fold more potent than MMDX and doxorubicin, respectively [1].

in vivo: An evaluation of the in vivo antitumor activity of PNU-

159682, in comparison with that of MMDX, was then conducted

in mice bearing disseminated murine L1210 leukemia.