产品描述:
CYT387 is an ATP-competitive inhibitor of the Janus kinases JAK1 and JAK2 (IC50s = 11 and 18 nM, respectively).{28486,27397} It displays significantly less activity against other kinases, including JAK3 (IC50 = 0.16 µM).{28486} At 0.5 to 1.5 µM, CYT387 causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines.{28486} It is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms, although kinase domain mutations can confer resistance.{28486,28485} CYT387 also blocks paclitaxel-induced JAK2 activation in ovarian cancer cells, preventing the development of a cancer stem cell-like population following chemotherapy.{28484}