Article
TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations.
Leukemia - 1 Aug 2007
Pardanani A, Hood J, Lasho T, Levine R L, Martin M B, Noronha G, Finke C, Mak C C, Mesa R, Zhu H, Soll R, Gilliland D G, Tefferi A
Abstract excerpt
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 (IC(50)=6 nM), FLT3 (IC(50)=25 nM) and RET (IC(50)=17 nM) kinases, with significantly less activity against other tyrosine kinases...
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