TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM, less potent to Flt3 and RET with IC50 of 25 nM and 17 nM, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations.
TG101209 is a potent inhibitor of the tyrosine kinases janus kinase (JAK) 2, FMS-like tyrosine kinase 3, proto-oncogene Ret, and JAK3 (IC50 = 6, 25, 17, and 169 nM, respectively).Through these effects, it induces cell cycle arrest and apoptosis in leukemic cell lines and CD45+ myeloma cells. |
