PNU-159682

202350-68-3

C32H35NO13

H2O : < 0.1 mg/mL (insoluble); DMSO : >= 100 mg/mL (155.86 mM)

Antibody-drug Conjugate/ADC Related

PNU-159682, a highly potent metabolite of the anthracycline nemorubicin with outstanding cytotoxicity, is a potent ADCs cytotoxin. In Vitro: PNU-159682 inhibits a panel of human tumor cell lines with IC₇₀ values in the range of 0.07-0.58 nM, and is 2, 360- to 790-fold and 6, 420- to 2, 100-fold more potent than MMDX and doxorubicin, respectively^[1]. PNU-159682 (100 uM) weakly inhibits topoisomerase II unknotting activity. PNU-159682 (10 uM)-DNA adducts contain one or two drug molecules bound to double-stranded DNA^[2]. PNU-159682 shows cytotoxic effect on CAIX-expressing SKRC-52 cells with IC₅₀ of 25 nM^[3]. In Vivo: PNU-159682 (15 ug/kg, i.v.) shows antitumor activity in mice bearing disseminated murine L1210 leukemia and in MX-1 human mammary carcinoma xenografts at 4 ug/kg^[1]. PNU-159682 (25 nmol/kg) exhibits a potent antitumor effect in mice bearing SKRC-52 xenografted tumors^[3].