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SYUIQ-5

Cat. No. M8179
SYUIQ-5 Structure
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Biological Activity

SYUIQ-5 is a Cryptolepine derivative, which induces and stabilizes G-quadruplexes. In CNE2 and HeLa cancer cells SYUIQ-5 triggers rapid and potent telomere DNA damage through TRF2 delocalization from telomeres and induces cell death by autophagy. In low concentration the compound caused senescence and telomere shortening. It is a potent cytotoxic agent.

Chemical Information
Molecular Weight 318.42
Formula C20H22N4
CAS Number 188630-47-9
Solubility (25°C) DMSO: ≥20 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] Yoanes Maria Vianney, et al. Indoloquinoline Ligands Favor Intercalation at Quadruplex-Duplex Interfaces

[2] Wen-Jun Zhou, et al. G-quadruplex ligand SYUIQ-5 induces autophagy by telomere damage and TRF2 delocalization in cancer cells

[3] Wen-Jun Zhou, et al. A G-quadruplex ligand SYUIQ-5 induces autophagy by inhibiting the Akt-FOXO3a pathway in nasopharyngeal cancer cells

[4] Qi-Biao Su, et al. Biotransformation and pharmacokinetics of the novel anticancer drug, SYUIQ-5, in the rat

[5] Qi-Biao Su, et al. High performance liquid chromatography with ultraviolet detection for the determination of SYUIQ-5, a novel telomerase inhibitor for cancer therapy: application to an enzyme kinetic study in rat liver microsomes

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