JAK1 inhibitor AZ-3

Chemical Structure : JAK1 inhibitor AZ-3

Catalog No.: PC-26419Not For Human Use, Lab Use Only.

JAK1 inhibitor AZ-3 is a potent, selective and orally efficacious JAK1 inhibitor with IC50 of 3.4 nM, >1000-fold selective over JAK2 , JAK3 and TYK2.

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Biological Activity

JAK1 inhibitor AZ-3 is a potent, selective and orally efficacious JAK1 inhibitor with IC50 of 3.4 nM, >1000-fold selective over JAK2 , JAK3 and TYK2.
AZ-3 exhibits potent inhibition of pSTAT3 in NCI-H1975 cells with IC50 of 30 nM.
AZ-3 (1, 3, 10, 30, 50, and 100 mg/kg, oral gavage) induced a dose-dependent decrease in pSTAT3 in NCI-H1975 mouse xenograft model.

Physicochemical Properties

M.Wt	385.49
Formula	C20H28FN7
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	N4-((R)-sec-butyl)-N2-(2-fluoro-5-((1S,4S)-5-methyl-2,5-diazabicyclo[2.2.1]heptan-2-yl)pyridin-3-yl)-5-methylpyrimidine-2,4-diamine

References

1. Grimster NP, et al. J Med Chem. 2018 Jun 28;61(12):5235-5244.

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