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Edecesertib

Chemical Structure : Edecesertib

CAS No.: 2408839-73-4

Edecesertib (GS-5718, GS5718)

Catalog No.: PC-22269Not For Human Use, Lab Use Only.

Edecesertib (GS-5718) is a potent, selective, and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with IC50 of 0.6 nM.

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Biological Activity

Edecesertib (GS-5718) is a potent, selective, and orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with IC50 of 0.6 nM.
Edecesertib (GS-5718) displays good potency in a human whole blood cellular assay (EC50 = 124 nM).
Edecesertib (GS-5718) is 123-fold less potent for IRAK1 and  >500-fold selectivity over a panel of kinases.
Edecesertib (GS-5718) demonstrated efficacy in a mouse NZB lupus model.

Physicochemical Properties

M.Wt 435.46
Formula C22H22FN7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-[[(1R)-1-Cyanoethyl]amino]-6-(3-cyanopyrrolo[1,2-b]pyridazin-7-yl)-N-[(2R)-2-fluoro-3-hydroxy-3-methylbutyl]-3-pyridinecarboxamide

References

1. Patent WO2020014468 A1.
2, Ammann SE, et al. J Med Chem. 2025 May 15. doi: 10.1021/acs.jmedchem.5c00463.

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