Definition
ChEBI: TG101209 is a member of the class of pyrimidines that is 5-methylpyrimidine-2,4-diamine in which the amino group at position 2 is substituted by a p-(4-methylpiperazin-1-yl)phenyl group, while that at position 4 is substituted by a m-(tert-butylsulfamoyl)phenyl group. A Janus kinase 2 (JAK2) inhibitor. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, an apoptosis inducer and an antineoplastic agent. It is a sulfonamide, a member of pyrimidines, a N-alkylpiperazine, a N-arylpiperazine and a secondary amino compound.
Biological Activity
tg101209, a small-molecule identified by structure based design, is a selective inhibitor of janus kinase 2 (jak2) that potently inhibits jak/stat pathway in multiple myeloma (mm) cell lines, such as cell harboring jak2v617f or mplw515l/k mutations which are commonly associated with polycythemia vera (pv) and primary myelofibrosis (pmf) respectively. according to results of multiple studies, it has revealed that tg101209 exhibits a dose and time dependent cyctoxicity, which is associated with inhibited cell cycle progrgression and induced apoptosis, in a wild range of mm cell lines through suppressing the expression of pjak2, pstat3 and bcl-xl and inducing the overexpression of perk and pakt.ramakrishnan v, kimlinger t, haug j, timm m, wellik l, halling t, pardanani a, tefferi a, rajkumar sv, kumar s. tg101209, a novel jak2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for cd45+ myeloma cells. am j hematol. 2010;85(9):675-686.
