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December 8, 2025BloodOpen Access

Identification of novel, potent, and selective JAK2V617F inhibitors

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Authors

PLPeter LindersAPAdeline PalisseRRRyan M. Richards

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Overview

Novel inhibitors significantly reduce JAK2V617F activity in hematological cancer, highlighting potential for improved therapeutic selectivity.

Key Points

  • Potent selective JAK2V617F inhibitors were identified, significantly reducing oncogenic signaling in MPNs.
  • Compounds exhibited over 10-fold selectivity over wild-type JAK2 in cell proliferation assays.
  • Assessment using biochemical probe displacement assays revealed sub-nanomolar potency in targeting the JAK2V617F variant.
  • Promising in vivo pharmacokinetic profiles suggest potential for clinical application in JAK2-driven malignancies.

Cite This Study

Linders et al. (2025) studied this question.

synapsesocial.com/papers/69362f444fa91c937236d5f2https://doi.org/10.1182/blood-2025-4326
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