TG-101348 is a potent, highly selective JAK2 inhibitor.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Tyrosine-protein kinase JAK2 inhibitor
Note
卖完停产，不再备货
Product Description
TG-101348 (SAR302503) is a selective inhibitor of JAK2 with IC50 of 3 nM, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3, TG-101348 also inhibit BRD4 with IC50 of 340 nM. A selective inhibitor of JAK2 tyrosine kinase
1.Wernig G, Kharas MG, Okabe R, Moore SA, Leeman DS, Cullen DE, Gozo M, McDowell EP, Levine RL, Doukas J et al.. (2008) Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia vera.. Cancer Cell, 13 (4):(311-20). [PMID:18394554]
2.Ciceri P, Müller S, O'Mahony A, Fedorov O, Filippakopoulos P, Hunt JP, Lasater EA, Pallares G, Picaud S, Wells C et al.. (2014) Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.. Nat Chem Biol, 10 (4):(305-12). [PMID:24584101]
3.Bose P, Alfayez M, Verstovsek S. (2019) New Concepts of Treatment for Patients with Myelofibrosis.. Curr Treat Options Oncol, 20 (1):(5). [PMID:30675650]
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E1718007