Cerdulatinib HCl is a dual JAK/SYK inhibitor with IC50 of 12 nM/6 nM/8 nM/0.5 nM and 32 nM for JAK1/JAK2/JAK3/TYK2 and Syk, respectively. It also inhibits other kinases with IC50 less than 200 nM.
Cerdulatinib hydrochloride (PRT062070) is a selective, orally bioavailable, and reversible ATP-competitive inhibitor targeting both SYK and JAK kinases, with IC50 values of 32 nM for SYK, and impressively low IC50s of 0.5 nM, 12 nM, 6 nM, and 8 nM for Tyk2, JAK1, JAK2, and JAK3, respectively. This dual inhibition profile positions cerdulatinib hydrochloride as a promising candidate for the study of autoimmune diseases and B-cell malignancies[1].[2].
Cerdulatinib HCl 动物研究
Animal study
In vivo, cerdulatinib administered orally at doses ranging from 0.5 to 5 mg/kg twice daily for two weeks demonstrates dose-dependent effectiveness in mitigating symptoms of collagen-induced arthritis (CIA) in rats. Additionally, cerdulatinib treatment in mice, at a dose not specified, twice daily for five days, effectively blocks BCR-induced B-cell activation and the resultant splenomegaly.
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