GSK854 is a potent TNNI3K 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%).
MedKoo Cat#: 555197
Name: GSK854
CAS#: 1316059-00-3
Chemical Formula: C18H19ClN6O4S2
Exact Mass: 482.0598
Molecular Weight: 482.96
Elemental Analysis: C, 44.77; H, 3.97; Cl, 7.34; N, 17.40; O, 13.25; S, 13.28
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| Soluble in DMSO | 0.0 | 100.00 |
The following data is based on the product molecular weight 482.96 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
