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Background Information:
TG101348 is a potent, selective and orally active inhibitor of JAK2 (IC50 = 3 nM). It has a 35- and 334-fold selectivity over JAK3 and JAK1, respectively. It is currently in clinical trials.
Reference:
1. Gerlinde Wernig, Michael G. Kharas, Rachel Okabe, et al., Efficacy of TG101348, a Selective JAK2 Inhibitor, in Treatment of a Murine Model of JAK2V617F-Induced Polycythemia Vera, Cancer Cell, 13(4): 311-320, 2008.
2. T Lasho, A Tefferi and A Pardanani, Inhibition of JAK–STAT signaling by TG101348: a novel mechanism for inhibition of KITD816V-dependent growth in mast cell leukemia cells, Leukemia 24, 1378-1380 (July 2010).
APIM050247: TG101348 (FEDRATINIB, SAR302503)
CAS No.: 936091-26-8.
Molecular Formula: C27H36N6O3S.
Molecular Weight: 524.7.
Purity: >99% (HPLC at 220 and 254 nm).
QC: HPLC, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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