Target Validation Information
TTD ID T08391
Target Name Janus kinase 2 (JAK-2)
Type of Target
Successful
Drug Potency against Target ITF2357 Drug Info IC50 = 1~10 nM [3]
Ruxolitinib Drug Info IC50 = 4.5 nM
Atropisomer 1 Drug Info IC50 = 270 nM [1]
NSC-1771 Drug Info IC50 = 223 nM [2]
Action against Disease Model ITF2357 Drug Info The clonogenic activity of JAK2V617F mutated cells was inhibited by low concentrations of ITF2357 (IC50 0.001-0.01 mu M) [3]
References
REF 1 Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole. J Med Chem. 2009 Dec 24;52(24):7938-41.
REF 2 In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
REF 3 The histone deacetylase inhibitor ITF2357 selectively targets cells bearing mutated JAK2(V617F). Leukemia. 2008 Apr;22(4):740-7.

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