TG101209

An inhibitor of JAK2, FLT3, RET, and JAK3

TG101209 is a potent inhibitor of the tyrosine kinases janus kinase (JAK) 2, FMS-like tyrosine kinase 3, proto-oncogene RET, and JAK3 (IC50 = 6, 25, 17, and 169 nM, respectively).1 Through these effects, it induces cell cycle arrest and apoptosis in leukemic cell lines and CD45+ myeloma cells.1,2

509.7

≥98%

CC(C)(C)NS(C1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2C)=C1)(=O)=O

C26H35N7O2S

936091-14-4

≥ 4 years

DMF: 16 mg/ml DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml DMSO: 12.5 mg/ml Ethanol: 0.12 mg/ml

1.Pardanani, A.,Lasho, T.,Levine, R.L., et al. TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia 21(8), 1658-1668 (2007).
2.Ramakrishnan, V.,Kimlinger, T.,Haug, J., et al. TG101209, a novel JAK2 inhibitor, has significant in-vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells. American Journal of Hematology 85(9), 675-686 (2010).