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PNU-159682 is a highly potent metabolite of the anthracycline nemorubicin (DNA topoisomerase II inhibitor) with outstanding cytotoxicity. PNU-159682 acts as a more potent and tolerated ADC cytotoxin than Doxorubicin for ADC synthesis. PNU-159682 is more potent than MMAE on NHL cell lines. In a cell viability assay, PNU-159682 is against BJAB.Luc, Granta-519, SuDHL4.Luc, and WSU-DLCL2 with IC50 values of 0.10 nM, 0.020 nM, 0.055 nM, and 0.1 nM, respectively. While MMAE is against BJAB.Luc, Granta-519, SuDHL4.Luc, and WSU-DLCL2 with IC50 values of 0.54 nM, 0.25 nM, 1.19 nM and 0.25 nM, respectively.
PNU-159682 (i.v.15 μg/kg; single-dose) is a maximum tolerated dose in murine L1210 leukemia model. PNU-159682 shows an improved antitumor activity in vivo. The antitumor effect of PNU-159682 (increase in life span=29%) is comparable to that afforded by 90 μg/kg MMDX (increase in life=36%). PNU-159682 (i.v. 4 μg/kg; 40 days) has a therapeutic response in MX-1 human mammary carcinoma mice. What’s more, from day 39, four out of seven mice receiving PNU-159682 exhibits complete tumor regression.
| Molecular Weight | 641.62 |
| Formula | C32H35NO13 |
| CAS Number | 202350-68-3 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage | 2-8°C, protect from light, sealed |
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