TG101348, 1 mg

Supplied by STEMCELL Technologies as a crystalline solid, this compound is a JAK/STAT pathway inhibitor that acts on JAK2 and related kinases. It inhibits Janus kinase 2 (JAK2) with an IC50 of 6 nM, and also blocks the related kinases Fms-related tyrosine kinase 3 (FLT3), RET, and JAK3 with IC50 values of 25, 17, and 169 nM, respectively. The molecule is proposed to bind to the ATP binding pocket of its kinase targets.

According to the manufacturer, the product is stable at -20°C as supplied, and small molecules should be stored away from direct light. For long-term storage, keep the material with a desiccant. Reported solubility is ≤ 95 mM in DMSO and ≤ 1 mM in absolute ethanol, and the compound has low solubility in aqueous media. When used as a cell culture supplement, stock solution should be diluted into culture medium immediately before use, with final DMSO concentration kept below 0.1% due to potential cell toxicity.

Published cancer research applications include suppression of growth in Ba/F3 cells expressing JAK2 V617F or MPL W515L mutations, reduced tumor cell burden and increased survival in mouse models of JAK2 V617F-induced hematopoietic and myeloproliferative disease, sensitization of erlotinib-resistant non-small cell lung cancer cells to erlotinib treatment in vitro and in mouse xenograft models, and displacement of BRD4 from chromatin with suppression of c-MYC expression in multiple myeloma cells in vitro. Alternative names listed include Fedratinib and SAR302503. The chemical formula is C27H36N6O3S, molecular weight is 524.7 g/mol, and purity is ≥ 98%.