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4E1RCat

Cat. No. M2360
4E1RCat Structure
Size Price Availability Quantity
5mg USD 86  USD86 In stock
10mg USD 118  USD118 In stock
50mg USD 270  USD270 In stock
100mg USD 480  USD480 In stock
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Quality Control & Documentation
Biological Activity

4E1RCat is a dual inhibitor of eIF4E:eIF4G and eIF4E:4E-BP1 interaction, and inhibits the binding of eIF4G to eIF4E with IC50 of 3.2 μM.

Chemical Information
Molecular Weight 478.45
Formula C28H18N2O6
CAS Number 328998-25-0
Form Solid
Solubility (25°C) DMSO 80 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] Yutaka Takaoka, et al. In Silico Drug Repurposing by Structural Alteration after Induced Fit: Discovery of a Candidate Agent for Recovery of Nucleotide Excision Repair in Xeroderma Pigmentosum Group D Mutant (R683W)

[2] Chao Fang, et al. eIF4E-eIF4G complex inhibition synergistically enhances the effect of sorafenib in hepatocellular carcinoma

[3] Shahzaib Ahamad, et al. Targeting SARS-CoV-2 nucleocapsid oligomerization: Insights from molecular docking and molecular dynamics simulations

[4] Gregory R Kardos, et al. Salubrinal in Combination With 4E1RCat Synergistically Impairs Melanoma Development by Disrupting the Protein Synthetic Machinery

[5] Nicholas Arnold, et al. Regulation of cardiac expression of the diabetic marker microRNA miR-29

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