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Cellagen Technology
JAK2/3 inhibitor
TG101209 is an orally-available, diaminopyrimidine-based inhibitor of JAK2 and Flt3 with IC50 values of 6, 25, and 17 nM, respectively. [1] In a human JAK2V617F-expressing acute myeloid leukemia cell line, TG101209 induced cell cycle arrest (G0/G1) and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5, and STAT3 at doses between 300-600 nM. In MM1S cells, however, a time-dependent cell cycle arrest was observed in the G2/M stages. [2]
TG101209 was recently utilized in studying a novel BCR-JAK2 tyrosine kinase in which the BCR oligomerization domain is fused to the JAK2 tyrosine-kinase domain. [3]
In lung cancers, TG101209 was shown to inhibit STAT3 activation and survivin expression, and sensitized HCC2429 and H460 cells to radation in clonogenic assays. [4]
Cellagen Technology
JAK2/3 inhibitor
TG101209 is an orally-available, diaminopyrimidine-based inhibitor of JAK2 and Flt3 with IC50 values of 6, 25, and 17 nM, respectively. [1] In a human JAK2V617F-expressing acute myeloid leukemia cell line, TG101209 induced cell cycle arrest (G0/G1) and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5, and STAT3 at doses between 300-600 nM. In MM1S cells, however, a time-dependent cell cycle arrest was observed in the G2/M stages. [2]
TG101209 was recently utilized in studying a novel BCR-JAK2 tyrosine kinase in which the BCR oligomerization domain is fused to the JAK2 tyrosine-kinase domain. [3]
In lung cancers, TG101209 was shown to inhibit STAT3 activation and survivin expression, and sensitized HCC2429 and H460 cells to radation in clonogenic assays. [4]
