| Name | PNU-159682 |
| Description | PNU-159682, a metabolite of anthracycline nemorubicin, is a DNA topoisomerase II inhibitor with excellent cytotoxicity. |
| In vitro | 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]. |
| In vivo | 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 96.7 mg/mL (150.71 mM), Sonication is recommended. 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (5.14 mM), Sonication is recommended.
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| Keywords | topoisomerase I | Topoisomerase | PNU-159682 | PNU159682 | PNU 159682 | non-Hodgkin's lymphoma | NMS249 | NHL | Inhibitor | inhibit | EDV nanocell | Daunorubicins/Doxorubicins | AML | ADCs Toxin | ADCCytotoxin | ADC Payload | ADC Cytotoxin | acute myeloid leukemia |
| Inhibitors Related | Ciprofloxacin hydrochloride monohydrate | Levofloxacin hydrochloride | Norfloxacin | Anthraquinone | Methotrexate disodium | Prulifloxacin | 1,4-Naphthoquinone | Ofloxacin | Levofloxacin | Dexamethasone | 3-Hydroxypyridine | Etoposide |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Bioactive Compound Library | Multi-Target Compound Library | Inhibitor Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |