TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations

@article{Pardanani2007TG101209AS,
  title={TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations},
  author={Animesh D Pardanani and John D. Hood and T L Lasho and R L Levine and M B Martin and Glenn Noronha and C M Finke and C C Mak and Ruben A Mesa and H Zhu and Richard M. Soll and D. Gary Gilliland and Ayalew Tefferi},
  journal={Leukemia},
  year={2007},
  volume={21},
  pages={1658-1668}
}
JAK2V617F and MPLW515L/K represent recently identified mutations in myeloproliferative disorders (MPD) that cause dysregulated JAK-STAT signaling, which is implicated in MPD pathogenesis. We developed TG101209, an orally bioavailable small molecule that potently inhibits JAK2 (IC50=6 nM), FLT3 (IC50=25 nM) and RET (IC50=17 nM) kinases, with significantly less activity against other tyrosine kinases including JAK3 (IC50=169 nM). TG101209 inhibited growth of Ba/F3 cells expressing JAK2V617F or… 
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TLDR
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