TG101209

TG101209 is a potent and small molecule JAK2-selective kinase inhibitor with IC50 of 6, 25, 17 and 169 nM for JAK2, FLT3, RET and JAK3, respectively.TG101209 potently prevents myeloproliferative disorder-related JAK2V617F and MPLW515L/K mutations. Besides, TG101209 suppressed the activation of STAT3 and survivin expression and sensitized HCC2429 and H460 cells to radiation in clonogenic assays. Immunohistochemistry staining of tumor sections showed that TG101209 enhanced apoptosis and decreased cell proliferation and vascular density, suggesting that TG101209 also has antiangiogenic effects.