TG101348, 10 mg

Offered by STEMCELL Technologies, this small molecule acts as an inhibitor of Janus kinase 2 (JAK2) within the JAK/STAT signaling pathway, with a reported IC50 of 6 nM. It also inhibits the related kinases fms-related tyrosine kinase 3 (FLT3), RET, and JAK3, with reported IC50 values of 25 nM, 17 nM, and 169 nM, respectively, and is proposed to bind to the ATP binding pocket of its kinase targets. The compound is supplied as a crystalline solid with a chemical formula of C27H36N6O3S, a molecular weight of 524.7 g/mol, and a purity of ≥ 98%. Alternative names for the compound include Fedratinib and SAR302503, and it has a CAS number of 936091-26-8.

In published cancer research studies, this JAK2 inhibitor has been reported to inhibit growth of Ba/F3 cells expressing JAK2 V617F or MPL W515L mutations, reduce tumor cell burden and increase survival in mouse models of JAK2 V617F-induced hematopoietic and myeloproliferative disease, sensitize erlotinib-resistant non-small cell lung cancer cells to erlotinib treatment in vitro and in a mouse xenograft model, and displace BRD4 from chromatin while suppressing c-MYC expression in multiple myeloma cells in vitro.