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Overview
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Background
TG101348, also known as SAR302503, is a potent and selective inhibitor of janus kinase 2 (JAK2), one member of a family of 4 cytoplasmic tyrosine kinases including janus kinase 1(JAK1), JAK2, janus kinase 3 (JAK3) and tyrosine kinase 2 (Tyk2), with the inhibition constant IC50 of 3 nM. Comparing to other close related kinases, the selectivity of TG101348 for JAK2 is 35- and 334-fold stronger than that for JAK3 and JAK1 respectively. TG10348 is capable of inducing apoptosis in HEL cells as well BaF/3 cells harboring JAK2V617 mutation and inhibiting hematopoietic progenitor colony formation and erythroid engraftment in samples from polycythemia vera (PV) patients.
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Overview