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PNU-159682

Cat. No. M10407
PNU-159682 Structure
Synonym:

PNU159682; metabolite of nemorubicin (MMDX)

Size Price Availability
5mg USD 750  USD750 Custom Synthesis
10mg USD 1000  USD1000 Custom Synthesis
25mg USD 1800  USD1800 Custom Synthesis
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Quality Control
  • Current batch:
  • Purity >97%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 641.62
Formula C32H35NO13
CAS Number 202350-68-3
Purity >97%
Solubility DMSO ≥ 90 mg/mL
Storage 2-8°C, protect from light, sealed
References

[1] Samuele Cazzamalli, et al. Mol Cancer Ther. Acetazolamide Serves as Selective Delivery Vehicle for Dipeptide-Linked Dгυgs to Renal Cell Carcinoma

[2] Luigi Quintieri, et al. Clin Cancer Res. Formation and antitumor activity of PNU-159682, a major metabolite of nemorubicin in human liver microsomes

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PNU-159682, PNU159682; metabolite of nemorubicin (MMDX) supplier, Topoisomerase, inhibitors

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