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AQ4

Cat. No. M7616
AQ4 Structure
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Biological Activity

AQ4 is a chemically stable cytotoxic agent used as a topoisomerase II inhibitor and DNA intercalator. The compound is a potent cytotoxic agent in many human tumor lines, including those derived from human pancreatic adenocarcinoma. Compound N - oxide is a hypoxic-activated topoisomerase targeting precursor compound.

Chemical Information
Molecular Weight 412.48
Formula C22H28N4O4
CAS Number 70476-63-0
Solubility (25°C) DMSO: ≥10 mg/mL
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] Maarten J Titulaer, et al. Overlapping demyelinating syndromes and anti–N-methyl-D-aspartate receptor encephalitis

[2] Edjah K Nduom, et al. Characterization of the blood-brain barrier of metastatic and primary malignant neoplasms

[3] Kaye J Williams, et al. In vivo activation of the hypoxia-targeted cytotoxin AQ4N in human tumor xenografts

[4] Swita Raghava, et al. AQ4, an antitumor anthracenedione, inhibits endothelial cell proliferation and vascular endothelial growth factor secretion: implications for the therapy of ocular neovascular disorders

[5] Sally J Atkinson, et al. Examination of the distribution of the bioreductive drug AQ4N and its active metabolite AQ4 in solid tumours by imaging matrix-assisted laser desorption/ionisation mass spectrometry

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Keywords: AQ4 supplier, inhibitors, activators


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