SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies

@article{Hart2011SB1518AN,
  title={SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies},
  author={S. Hart and K. Goh and V. Novotny‐Diermayr and C. Hu and H. Hentze and Y. C. Tan and B. Madan and C. Amalini and Y. Loh and L. Ong and A. William and A. Lee and A. Poulsen and R. Jayaraman and K. Ong and K. Ethirajulu and B. Dymock and J. Wood},
  journal={Leukemia},
  year={2011},
  volume={25},
  pages={1751-1759}
}
SB1518 is an innovative pyrimidine-based macrocycle that shows a unique kinase profile with selective inhibition of Janus Kinase-2 (JAK2; IC50=23 and 19 nM for JAK2WT and JAK2V617F, respectively) within the JAK family (IC50=1280, 520 and 50 nM for JAK1, JK3 and TYK2, respectively) and fms-like tyrosine kinase-3 (FLT3; IC50=22 nM). SB1518 shows potent effects on cellular JAK/STAT pathways, inhibiting tyrosine phosphorylation on JAK2 (Y221) and downstream STATs. As a consequence SB1518 has potent… Expand
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