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Briciclib

Cat. No. M20585
Briciclib Structure
Synonym:

ON-014185

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Biological Activity

Briciclib is a water soluble derivative of ON-013100, a small molecule that binds to and inhibits eukaryotic translation initiation factor 4E (eIF4E) .

Chemical Information
Molecular Weight 474.42
Formula C19H23O10PS
CAS Number 865783-99-9
Solubility (25°C) DMSO 95 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] Khaled M Elattar, et al. Curr Org Synth. Bicyclic 5-6 Systems: Comprehensive Synthetic Strategies for the Annulations of Pyrazolo[ 1,5-a]pyrimidines

[2] Shuai Wang, et al. Eur J Med Chem. FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application

[3] Shahrzad Ahangarzadeh, et al. Drug Discov Today. Bicyclic peptides: types, synthesis and applications

[4] Elena Lenci, et al. Org Biomol Chem. Bicyclic acetals: biological relevance, scaffold analysis, and applications in diversity-oriented synthesis

[5] Curran A Rhodes, et al. Chemistry. Bicyclic Peptides as Next-Generation Therapeutics

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Keywords: Briciclib, ON-014185 supplier, inhibitors, activators


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