TG101348 is an inhibitor of Janus kinase 2 (JAK2) with an IC50 of 6 nM
It also inhibits related kinases fms-related tyrosine kinase 3 (FLT3), RET, and JAK3 with less potent activity, having IC50 values of 25, 17 and 169 nM, respectively (Pardanani et al.) It is proposed to bind to the ATP binding pocket of its kinase targets (Zhou et al.)
Inhibits growth of Ba/F3 cells expressing JAK2 V617F or MPL W515L mutations (Pardanani et al.)
Reduces tumor cell burden and increases survival in mouse models of JAK2 V617F-induced hematopoietic and myeloproliferative disease (Pardanani et al.; Wernig et al.)
Sensitizes erlotinib-resistant non-small cell lung cancer cells to erlotinib treatment in vitro and in a mouse xenograft model (Zhang et al.)
Displaces BRD4 from chromatin and suppresses c-MYC expression in multiple myeloma cells in vitro (Ciceri et al.)
