Discovery of Highly Selective and Potent Macrocyclic JAK2 Inhibitors for the Treatment of MPNs

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Novel macrocyclic jak2 inhibitors improve selectivity and efficacy in mPN models, implying better treatment outcomes.

Compound 15au demonstrates potent jak2 inhibition with an IC50 of 2 nM, showing significant therapeutic promise.
Inhibition results in enhanced kinase selectivity, boasting 89.5-fold selectivity over jak1, improving treatment targeting.
The macrocyclization strategy effectively refines jak2 inhibitors, enhancing metabolic stability and overall efficacy.
15au outperforms existing therapies like pacritinib at lower doses, indicating potential clinical advantages for mPN treatment.

Qin et al. (2025) studied this question.

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View Full Paper

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Authors

Novel macrocyclic jak2 inhibitors improve selectivity and efficacy in mPN models, implying better treatment outcomes.

Compound 15au demonstrates potent jak2 inhibition with an IC50 of 2 nM, showing significant therapeutic promise.
Inhibition results in enhanced kinase selectivity, boasting 89.5-fold selectivity over jak1, improving treatment targeting.
The macrocyclization strategy effectively refines jak2 inhibitors, enhancing metabolic stability and overall efficacy.
15au outperforms existing therapies like pacritinib at lower doses, indicating potential clinical advantages for mPN treatment.

Qin et al. (2025) studied this question.

View Full Paper

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