TG101348

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Description

TG101348 is a selective small-molecule Janus kinase 2 (JAK2) inhibitor with IC50 of 6 nM.TG-101348 also inhibits FLT3 and RET with IC50 values of 25 and 17 nM, respectively. In vivo, TG101348 exhibits promising pharmacokinetic profiles in species ranging from mouse to monkey including oral availabilities >20%, and half-lives consistent with once or twice daily dosing. TG101348 reduces the number of circulating mutant JAK2 cells, inhibited splenomegaly and improved survival without significantly impacting normal hematocrit in an aggressive JAK2-driven circulating cell model of disease in rodents.

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