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December 8, 2025BloodOpen Access

Preclinical characterization of a novel, wild-type-sparing, JAK2 V617F mutant-selective inhibitor

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Authors

MCMark J. ChicarelliMCMichelle CrowKAKim Alley

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Overview

Preclinical findings demonstrate that CGT1145 may effectively improve splenomegaly and tolerability in myeloproliferative neoplasms.

Key Points

  • This research aims to characterize the potential of the novel JAK2 V617F inhibitor CGT1145 in treating myeloproliferative neoplasms.
  • Preclinical characterization of CGT1145 through binding affinity and selectivity assays.
  • Cellular activity assessed using phospho-STAT5 readouts in JAK2 mutant and wild-type cell lines.
  • In vivo evaluation of CGT1145 in athymic nude mice implanted with JAK2 V617F cells.
  • CGT1145 demonstrated high selectivity and potency with an IC50 of 91nM for JAK2 V617F.
  • Target engagement resulted in robust inhibition of tumor phospho-STAT5 in mice.
  • CGT1145 showed improved tolerability compared to traditional treatments.

Cite This Study

Chicarelli et al. (2025) studied this question.

synapsesocial.com/papers/693624d74fa91c937236d11fhttps://doi.org/10.1182/blood-2025-3752
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