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PNU-159682, a metabolite of anthracycline neomycin, is a DNA topoisomerase II inhibitor with excellent cytotoxicity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $84 | In Stock | |
5 mg | $198 | In Stock | |
10 mg | $363 | In Stock | |
25 mg | $767 | In Stock | |
50 mg | $1,180 | In Stock | |
100 mg | $1,830 | In Stock |
Description | PNU-159682, a metabolite of anthracycline neomycin, is a DNA topoisomerase II inhibitor with excellent cytotoxicity. |
Targets&IC50 | CA IX:25 nM, Topo II unknotting activity:100 μM |
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]. |
Molecular Weight | 641.62 |
Formula | C32H35NO13 |
Cas No. | 202350-68-3 |
Smiles | CO[C@H]1OCCN2[C@H]3C[C@H](O[C@H]4C[C@@](O)(Cc5c(O)c6C(=O)c7cccc(OC)c7C(=O)c6c(O)c45)C(=O)CO)O[C@@H](C)[C@H]3O[C@H]12 |
Relative Density. | 1.58 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 96.7 mg/mL (150.71 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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