Janus kinases (JAKs) are non-receptor kinases that mediate signaling through cytokine receptors, often to members of the signal transducer and activator of transcription (STAT) family.{20362} JAK2V617F and MPLW515L/K are two known mutations that cause dysregulated JAK-STAT signaling in myeloproliferative disorders. TG101348 is a small molecule inhibitor of JAK2 (IC50 = 6 nM) and the related kinases FLT3 (IC50 = 25 nM) and RET (IC50 = 17 nM) with significantly less potent activity against JAK3 (IC50 = 169 nM).{23418} It can inhibit the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 value of 200 nM.{23418} Phase I clinical trial results that focused on safety and efficacy of TG101348 in patients with high- or intermediate-risk primary or post-polycythemia vera/essential thrombocythemia myelofibrosis have been published.{27682}
产品描述
A small molecule inhibitor of JAK2 (IC50 = 6 nM) and the related kinases FLT3 (IC50 = 25 nM) and RET (IC50 = 17 nM) with significantly less potent activity against JAK3 (IC50 = 169 nM); inhibits the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations (IC50 = 200 nM)
