GSK854 is a novel and potent TNNI3K (Troponin I-Interacting Kinase) inhibitor with IC50 (TNNI3K) < 10 nM. GSK854 exhibits substantial selectivity against B-Raf (>25-fold) and EGFR (IC50 > 25 μM), excellent broad spectrum kinase selectivity with >100-fold selectivity over 96% of kinases tested (≤50% inhibition @ 1 μM for 282 of 294 kinases, high activity in a TNNI3K cellular assay (IC50 = 8 nM), good pharmacokinetics in rats (Cl = 14 mL/min/kg, Vdss = 1.9 L/kg, t1/2 = 2.3 h, F =
48%).
纯度:≥98%
CAS:1316059-00-3