PNU-159682 是蒽环类新霉素的代谢产物，是一种 DNA 拓扑异构酶 II 抑制剂，具有出色的细胞毒性。

PNU-159682 is a highly effective metabolite of the anthracycline nemorubicin. PNU-159682 has outstanding cytotoxicity. PNU-159682 is an effective ADCs cytotoxin.

PNU-159682 inhibits a panel of human tumor cell lines (IC70 values in the range of 0.07-0.58 nM). PNU-159682 is 2,360- to 790-fold and 6,420- to 2,100-fold more potent than MMDX and doxorubicin, respectively. PNU-159682 displays cytotoxic effect on CAIX-expressing SKRC-52 cells (IC50: 25 nM). PNU-159682 (10 μM)-DNA adducts contain one or two drug molecules bound to double-stranded DNA. PNU-159682 (100 μM) weakly inhibits topoisomerase II unknotting activity [1][2][3].

PNU-159682 (25 nmol/kg) shows an effective antitumor effect in mice bearing SKRC-52 xenografted tumors. PNU-159682 (15 μg/kg, i.v.) displays antitumor activity in mice bearing disseminated murine L1210 leukemia and in MX-1 human mammary carcinoma xenografts at 4 μg/kg[1][3].

202350-68-3

C32H35NO13

641.62

DMSO:96.7 mg/mL (150.71 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years