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Nemorubicin

Cat. No. M27770
Nemorubicin Structure
Synonym:

Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243

Size Price Availability Quantity
5mg USD 132  USD132 In stock
10mg USD 240  USD240 In stock
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Quality Control & Documentation
Biological Activity

Nemorubicin (Methoxymorpholinyl doxorubicin) is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin not only intercalate into the duplex DNA, but also result in significant ligands for G-quadruplex DNA segments, stabilizing their structure. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity.

Chemical Information
Molecular Weight 643.64
Formula C32H37NO13
CAS Number 108852-90-0
Form Solid
Solubility (25°C) DMSO 65 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Matteo Scalabrin, et al. Chem Res Toxicol. Virtual Cross-Linking of the Active Nemorubicin Metabolite PNU-159682 to Double-Stranded DNA

[2] Leonardo Scaglioni, et al. Biochim Biophys Acta. Nemorubicin and doxorubicin bind the G-quadruplex sequences of the human telomeres and of the c-MYC promoter element Pu22

[3] Massimo Broggini. Top Curr Chem. Nemorubicin

[4] Stefania Mazzini, et al. Bioorg Med Chem. The interaction of nemorubicin metabolite PNU-159682 with DNA fragments d(CGTACG)(2), d(CGATCG)(2) and d(CGCGCG)(2) shows a strong but reversible binding to G:C base pairs

[5] Luigi Quintieri, et al. Biochem Pharmacol. In vitro hepatic conversion of the anticancer agent nemorubicin to its active metabolite PNU-159682 in mice, rats and dogs: a comparison with human liver microsomes

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Keywords: Nemorubicin, Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243 supplier, DNA/RNA Synthesis, inhibitors, activators


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