TG101348 (FEDRATINIB, SAR302503)

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.