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Quarfloxin

Cat. No. M13652
Quarfloxin Structure
Synonym:

CX-3543

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Biological Activity

Quarfloxin (CX-3543), a fluoroquinolone derivative with antineoplastic activity, targets and inhibits RNA pol I activity, with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template.

Chemical Information
Molecular Weight 604.67
CAS Number 865311-47-3
Solubility (25°C) Water 1 mg/mL (ultrasonic and adjust pH to 5 with 0.1 M HCL)
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] Josu Carvalho, et al. Trends Mol Med. G-quadruplex, Friend or Foe: The Role of the G-quartet in Anticancer Strategies

[2] Mingli Yang, et al. Curr Top Med Chem. Moxifloxacin-isatin Hybrids Tethered by 1,2,3-triazole and their Anticancer Activities

[3] Lynne M Harris, et al. Antimicrob Agents Chemother. G-Quadruplex DNA Motifs in the Malaria Parasite Plasmodium falciparum and Their Potential as Novel Antimalarial Drug Targets

[4] Louise E Kerry, et al. PLoS Negl Trop Dis. Selective inhibition of RNA polymerase I transcription as a potential approach to treat African trypanosomiasis

[5] Joanna Bidzinska, et al. Molecules. G-quadruplex structures in the human genome as novel therapeutic targets

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