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Pyridostatin

Cat. No. M27767
Pyridostatin Structure
Synonym:

RR82

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Biological Activity

Pyridostatin (RR82) is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin targets the proto-oncogene Src. Pyridostatin reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.

Chemical Information
Molecular Weight 596.64
Formula C31H32N8O5
CAS Number 1085412-37-8
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Liu-Yi Liu, et al. J Am Chem Soc. Structural Basis of Pyridostatin and Its Derivatives Specifically Binding to G-Quadruplexes

[2] Yinzhu Hou, et al. Nucleic Acids Res. G-quadruplex inducer/stabilizer pyridostatin targets SUB1 to promote cytotoxicity of a transplatinum complex

[3] Florian J Groelly, et al. EMBO Mol Med. Anti-tumoural activity of the G-quadruplex ligand pyridostatin against BRCA1/2-deficient tumours

[4] Min Zou, et al. Int J Biol Macromol. G-quadruplex binder pyridostatin as an effective multi-target ZIKV inhibitor

[5] Michele Olivieri, et al. Cell. A Genetic Map of the Response to DNA Damage in Human Cells

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Keywords: Pyridostatin, RR82 supplier, DNA/RNA Synthesis, inhibitors, activators


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