Cat No.
CEI-0194
Description
As a JAK2 selective inhibitor, TG101209 can inhibit JAK2 (IC50=6 nM), FLT3 (IC50=25 nM) and RET (IC50=17 nM) kinases and JAK3 (IC50=169 nM).
CAS No.
936091-14-4
Targets
JAK2, FLT3, RET
Chemical Name
N-tert-butyl-3-(5-methyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-ylamino)benzenesulfonamide
M.Wt
509.67
Purity
>99%
Solubility
DSMO 102 mg/mL Water
Storage
2 years at -20 centigrade
In vitro
As a JAK2 selective inhibitor, TG101209 can inhibit JAK2 (IC50=6 nM), FLT3 (IC50=25 nM) and RET (IC50=17 nM) kinases and JAK3 (IC50=169 nM). By inducing cell cycle arrest and apoptosis, and inhibiting phosphorylation of JAK2V617F, STAT5 and STAT3, TG101209 inhibit the cell proliferation of human JAK2V617F-expressing acute myeloid leukemia cell line. TG101209 inhibited growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 of 200 nM.TG101209 can induce cytotoxicity in a variety of multiple myeloma (MM) cell lines in dose- and time-dependent manners. TG101209 can induce apoptosis and inhibit cell cycle progression in myeloma cell lines and patient-derived plasma cells. Co-treatment with BEZ235 and JAK2-TKI (TG101209 and SAR302503) synergistically induced lethal activity against the cultured and primary CD34+ MPN cells while relatively sparing the normal CD34+ HPCs.
In vivo
Treatment with TG101209 not only prevented bleomycin-induced fibrosis but also effectively reduced skin fibrosis in TSK-1 mice. addition of TG101209 to radiation in lung xenografts produced a significant tumor growth delay (>10 days) compared with radiation alone and was well tolerated. TG101209 increased apoptosis and decreased cell proliferation and vascular density.
