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Biological Activity:
An orally bioavailable, ATP-competitive and selective inhibitor of Janus-associated kinase 2 (JAK2, IC50: ca 3 nM) with potential antineoplastic activity.
References: online 1 2 3
J Hood et al. TG101348, a potent, highly selective JAK2 inhibitor, inhibits colony formation in stem cells from polycythemia vera patients and prevents JAK2V617F-mediated splenomegaly and death in a mouse model. J. Clin. Oncol. (2007 ASCO Annual Meeting Proceedings Part I. Vol 25, No. 18S) 2007, 7031.
G Wernig et al. Efficacy of TG101348, a Selective JAK2 Inhibitor, in Treatment of a Murine Model of JAK2V617F-Induced Polycythemia Vera. Cancer Cell 2008, 13, 311–320. [online]
Chemical Name: (N-tert-butyl-3-(5-methyl-2-(4-(2-(pyrrolidin-1-yl)ethoxy)phenylamino)pyrimidin-4-ylamino)benzenesulfonamide
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