TG-101348 (Fedratinib, SAR302503) is a potent, selective JAK2 inhibitor with IC50 of 3 nM for both wt JAK2 and JAK2 V617F.
TG-101348 also inhibits FLT3 (IC50=15 nM) and RET (IC50=48 nM) kinases, weakly inhibits JAK3 (IC50=168 nM), >35-fold selectivity over JAK1/3 and Tyk2.
TG-101348 shows therapeutic efficacy in a murine model of myeloproliferative disease induced by the JAK2V617F mutation.
TG-101348 also potently inhibits BRD4 with Kd of 168 nM.
