Sample solution is provided at 25 µL, 10mM.
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|Description||TG101209 is a selective inhibitor of JAK2 with IC50 of 6 nM.|
|IC50||6 nM||25 nM||17 nM||169 nM|
|Cas No.||936091-14-4||SDF||Download SDF|
|Solubility||>25.5mg/mL in DMSO||Storage||Store at -20°C|
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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.